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Bcl-2

Isoform-selective Products

Bcl-2 Bcl-B Bcl-w Bcl-xL Mcl-1 Bax Bfl-1 Bad Bcl-xL

Signaling Pathway

Bcl-2 Products

All (59)
Bcl-2 Inhibitors (40)
Bcl-2 Activators (8)
Bcl-2 Antagonists (5)
Bcl-2 Modulators (5)
New Bcl-2 Products

Catalog No.	Product Name	Information	Product Use Citations
S8048	Venetoclax (ABT-199)	Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.	Nat Immunol, 2024, 10.1038/s41590-024-01952-4 J Hematol Oncol, 2024, 17(1):85 Nat Commun, 2024, 15(1):1821
S1002	ABT-737	ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.	Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Commun, 2024, 15(1):1041 Nat Commun, 2024, 15(1):830
S1001	Navitoclax (ABT-263)	Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.	Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Commun, 2024, 15(1):1041 Cell Rep Med, 2024, 5(3):101471
S7747	Ro-3306	RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.	Nat Commun, 2024, 15(1):2089 Nucleic Acids Res, 2024, gkae747 Nucleic Acids Res, 2024, gkae263
S1057	Obatoclax Mesylate (GX15-070)	Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.	bioRxiv, 2024, 10.1101/2023.01.18.524628 Emerg Microbes Infect, 2022, 1-29 Cancers (Basel), 2022, 14(22)5602
S8383	S63845	S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.	Cell Death Discov, 2024, 10(1):417 Cancer Sci, 2024, 10.1111/cas.16292 Biomolecules, 2024, 14(5)555
S7790	A-1210477	A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.	Cell Rep, 2023, 42(10):113176 Int J Mol Sci, 2023, 24(13)11149 Int J Mol Sci, 2023, 24(13)11149
S1121	TW-37	TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.	bioRxiv, 2024, 10.1101/2023.01.18.524628 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
S7801	A-1331852	A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.	Cell Death Dis, 2024, 15(5):323 Apoptosis, 2024, 10.1007/s10495-024-02014-8 Cell Death Discov, 2024, 10(1):417
S7800	A-1155463 Dihydrochloride	A-1155463 Dihydrochloride, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).	iScience, 2024, 27(1):108503 World J Oncol, 2024, 15(3):472-481 Cancer Res Commun, 2024, 4(4):1024-1040
S2606	Mifepristone	Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.	Neuron, 2024, S0896-6273(24)00089-8 Cell Death Dis, 2024, 15(1):70 Cell Death Dis, 2024, 15(1):73
S7531	UMI-77	UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	iScience, 2024, 27(1):108503 Blood, 2022, blood.2021014304 Nat Commun, 2022, 13(1):6226
S2812	(R)-(-)-Gossypol (AT-101) acetic acid	(R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.	Protein Cell, 2024, pwad065 Int J Mol Sci, 2023, 24(7)6662 Cancer Cell, 2022, S1535-6108(22)00312-9
S8643	AZD5991	AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Cell Death Discov, 2024, 10(1):175 Cell Rep, 2023, 42(10):113176 Cells, 2023, 12(18)2247
S8061	Sabutoclax	Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Mol Divers, 2022, 10.1007/s11030-022-10494-6
S7100	WEHI-539	WEHI-539 has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.	Cell Rep Med, 2023, 4(11):101290 Liver Int, 2022, 10.1111/liv.15392 Cell Death Differ, 2021, 10.1038/s41418-021-00816-w
S1071	HA14-1	HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.	Platelets, 2020, 10.1080/09537104.2020.1724276 Oncotarget, 2018, 9(24):16701-16717 Oncotarget, 2015, 6(34):36113-25
S8836	MIK665 (S64315)	MIK665 (S64315) is an inhibitor of induced myeloid leukemia cell differentiation protein Mcl-1 with Ki value of 1.2 nM and has potential pro-apoptotic and antineoplastic activities.	Nat Commun, 2024, 15(1):1581 Cell Rep, 2023, 42(10):113176 Biomedicines, 2023, 11(6)1666
S6709	Obatoclax (GX15-070)	Obatoclax (GX15-070) is an antagonist of Bcl-2 with an Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.	Oncotarget, 2024, 15:614-633 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
S8820	Unesbulin (PTC596)	Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.	NPJ Precis Oncol, 2024, 8(1):68 PLoS One, 2023, 18(2):e0277313 bioRxiv, 2023, 2023.01.23.525196
S2448	Gambogic Acid	Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Cancers (Basel), 2022, 14(22)5505
S7126	Marinopyrrole A (Maritoclax)	Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.	Clin Cancer Res, 2023, 29(2):446-457 Clin Cancer Res, 2023, 29(2):446-457 Cell Signal, 2022, S0898-6568(22)00041-9
S8865	BAI1	BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.	Int J Hyperthermia, 2024, 41(1):2325489 Nat Commun, 2023, 14(1):865 iScience, 2022, 25(10):105145
S6852	Gossypol	Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Mol Med Rep, 2021, 23(1)40
E2926	A-1155463	A-1155463 is a highly potent and selective BCL-XL inhibitor with EC50 of 65 nM in H146 cells.	Leukemia, 2024, 38(1):136-148 Br J Cancer, 2024, 10.1038/s41416-024-02740-5 Nat Commun, 2023, 14(1):4033
S8650	BTSA1	BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.	bioRxiv, 2024, 10.1101/2023.01.18.524628 Cell Mol Life Sci, 2023, 80(10):311 Cell Mol Life Sci, 2023, 80(10):311
S8759	S55746	S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Signal Transduct Target Ther, 2022, 7(1):51
S7105	BAM7	BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.	Nat Chem Biol, 2019, 15(4):322-330 Cell Death Discov, 2018, 4:107
S3275	Senkyunolide I	Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	World J Emerg Med, 2024, 15(3):206-213 SSRN , 2024, 10.2139/ssrn.4696834 Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
S5967	Berberine chloride hydrate	Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Biosci (Landmark Ed), 2022, 27(8):242 Front Pharmacol, 2021, 12:632201
S8199	Ruxotemitide (LTX 315)	Ruxotemitide (LTX 315) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.	J Immunother Cancer, 2022, 10(3)e004129 Nat Metab, 2021, 10.1038/s42255-021-00491-8
S7849	BDA-366	BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).	BMC Cancer, 2023, 23(1):479
S3238	Resibufogenin	Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.	Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S0563	10-Deacetyl-7-xylosyl paclitaxel	10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.	Cell Death Dis, 2022, 13-9:799
E0124	Chelerythrine	Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.	Nutr Neurosci, 2022, 1-19
E3037	Solanum lyratum Extract	Solanum lyratum Extract (300 μg/ml) increases Bax levels and decreases Bcl-2 levels, which cause the loss of mitochondrial membrane potential (Δæm) followed by cytochrome C release and caspase-9 and -3 activation, finally leading to apoptosis. Solanum lyratum Extract (300 μg/ml) also promotes p53 and p27, but decreases the levels of cyclin B1 thus causing S-phase arrest.
S3224	Cinobufagin	Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S6895	TCPOBOP	TCPOBOP is a constitutive androstane receptor (CAR) agonist. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
S9970	APG-2575 (lisaftoclax)	APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
S3245	Nodakenetin	Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3267	Nicotiflorin (Kaempferol-3-O-rutinoside)	Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
S3243	Zeaxanthin	Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
E2354	Valepotriate	Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
E2028	Humanin	Humanin (human) (1-24-Protein humanin (human)), a small mitochondrial-derived cytoprotective polypeptide encoded by mtDNA, exhibits protective effects in several cell types against cellular stress conditions and apoptosis through regulating various signaling mechanisms, such as JAK/STAT pathway and interaction of BCL-2 family of protein.
E0011	Linderalactone	Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
S9276	Alisol B	Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
E1510^New	Sonrotoclax	Sonrotoclax(BGB-11417) is a highly potent, orally active and selective inhibitor of Bcl2. Sonrotoclax demonstrates increased potency along with in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant. Bcl-xL Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712 J Biomol Struct Dyn, 2022, 1-11
S5600	Flavokawain A	Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S8177	BH3I-1	BH3I-1 is a Bcl-X_L-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.
S8924	DT2216	DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
S6004	CCI-007	CCI-007 is a novel small molecule with cytotoxic activity against infant leukemia with MLL rearrangements.
S9665	Motixafortide (BL-8040)	Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S8758	VU661013	VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
S5550	Ethyl gallate	Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. Ethyl gallat activates the death receptor-dependent pathway of apoptosis by enhancing the expression of caspases-8, -9, and -3 and the Bcl-2 interacting domain (Bid).
S8550^New	AMG-176	AMG 176(Tapotoclax, Tapotoclaxum) is a potent, selective, and orally bioavailable macrocyclic inhibitor of MCL1 with a Ki of 0.13 nM. It induces a potent apoptosis in models of hematologic malignancies.
S6990	Phytohemagglutinin (PHA)	Phytohemagglutinin (PHA) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.	Molecules, 2023, 28(6)2426
E2663	BT2	BT2 is a novel branched-chain α-ketoacid dehydrogenase complex kinase (BDK) inhibitor wieh an IC50 of 3.19 μM.
E3020	Hedyotic Diffusa Extract	Hedyotic Diffusa Extract is extracted from Hedyotic diffusa, of which polysaccharides inhibit the growth of CNE2 cells in a dose-and-time-dependent way, the mechanism may involve induction of cell apoptosis, which is associated with the activation of Bax and caspase-3 protein and the down-regulation of Bcl-2 protein expression.
S8048	Venetoclax (ABT-199)	Venetoclax (ABT-199, GDC-0199) is a Bcl-2-selective inhibitor with K_i of <0.01 nM in cell-free assays, >4800-fold more selective versus Bcl-xL and Bcl-w, and no activity to Mcl-1. Venetoclax is reported to induce cell growth suppression, apoptosis, cell cycle arrest, and autophagy in triple negative breast cancer MDA-MB-231 cells. Phase 3.	Nat Immunol, 2024, 10.1038/s41590-024-01952-4 J Hematol Oncol, 2024, 17(1):85 Nat Commun, 2024, 15(1):1821
S1002	ABT-737	ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1. ABT-737 induces mitochondrial pathway apoptosis and mitophagy. Phase 2.	Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Commun, 2024, 15(1):1041 Nat Commun, 2024, 15(1):830
S1001	Navitoclax (ABT-263)	Navitoclax (ABT-263) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with K_i of ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.	Gastroenterology, 2024, S0016-5085(24)00062-3 Nat Commun, 2024, 15(1):1041 Cell Rep Med, 2024, 5(3):101471
S8383	S63845	S63845 is a new, selective MCL-1 inhibitor with the Kd value of 0.19 nM and has no discernible binding to the other BCL-2 members, BCL-2 or BCL-XL.	Cell Death Discov, 2024, 10(1):417 Cancer Sci, 2024, 10.1111/cas.16292 Biomolecules, 2024, 14(5)555
S7790	A-1210477	A-1210477 is a potent and selective MCL-1 inhibitor with K_i and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.	Cell Rep, 2023, 42(10):113176 Int J Mol Sci, 2023, 24(13)11149 Int J Mol Sci, 2023, 24(13)11149
S1121	TW-37	TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.29 μM, 1.11 μM and 0.26 μM in cell-free assays, respectively.	bioRxiv, 2024, 10.1101/2023.01.18.524628 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
S7801	A-1331852	A-1331852 is a potent and selectiveBCL-XL inhibitor with Ki value less than 0.01 nM for BCL-XL and 6 nM, 4 nM, 142 nM for Bcl-2, Bcl-W, MCL-1 respectively. It may be useful in the treatment of cancer, immune and autoimmune diseases.	Cell Death Dis, 2024, 15(5):323 Apoptosis, 2024, 10.1007/s10495-024-02014-8 Cell Death Discov, 2024, 10(1):417
S7800	A-1155463 Dihydrochloride	A-1155463 Dihydrochloride, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).	iScience, 2024, 27(1):108503 World J Oncol, 2024, 15(3):472-481 Cancer Res Commun, 2024, 4(4):1024-1040
S2606	Mifepristone	Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.	Neuron, 2024, S0896-6273(24)00089-8 Cell Death Dis, 2024, 15(1):70 Cell Death Dis, 2024, 15(1):73
S7531	UMI-77	UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.	iScience, 2024, 27(1):108503 Blood, 2022, blood.2021014304 Nat Commun, 2022, 13(1):6226
S2812	(R)-(-)-Gossypol (AT-101) acetic acid	(R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with K_i of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.	Protein Cell, 2024, pwad065 Int J Mol Sci, 2023, 24(7)6662 Cancer Cell, 2022, S1535-6108(22)00312-9
S8643	AZD5991	AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.	Cell Death Discov, 2024, 10(1):175 Cell Rep, 2023, 42(10):113176 Cells, 2023, 12(18)2247
S8061	Sabutoclax	Sabutoclax (BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Mol Divers, 2022, 10.1007/s11030-022-10494-6
S1071	HA14-1	HA14-1 is a non-peptidic ligand of a Bcl-2 surface pocket with IC50 of ~9 μM.	Platelets, 2020, 10.1080/09537104.2020.1724276 Oncotarget, 2018, 9(24):16701-16717 Oncotarget, 2015, 6(34):36113-25
S8836	MIK665 (S64315)	MIK665 (S64315) is an inhibitor of induced myeloid leukemia cell differentiation protein Mcl-1 with Ki value of 1.2 nM and has potential pro-apoptotic and antineoplastic activities.	Nat Commun, 2024, 15(1):1581 Cell Rep, 2023, 42(10):113176 Biomedicines, 2023, 11(6)1666
S8820	Unesbulin (PTC596)	Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.	NPJ Precis Oncol, 2024, 8(1):68 PLoS One, 2023, 18(2):e0277313 bioRxiv, 2023, 2023.01.23.525196
S2448	Gambogic Acid	Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Cancers (Basel), 2022, 14(22)5505
S8865	BAI1	BAI1 is a direct allosteric inhibitor of BAX with a dissociation constant (Kd) of 15.0 ± 4 μM.	Int J Hyperthermia, 2024, 41(1):2325489 Nat Commun, 2023, 14(1):865 iScience, 2022, 25(10):105145
S6852	Gossypol	Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Mol Med Rep, 2021, 23(1)40
E2926	A-1155463	A-1155463 is a highly potent and selective BCL-XL inhibitor with EC50 of 65 nM in H146 cells.	Leukemia, 2024, 38(1):136-148 Br J Cancer, 2024, 10.1038/s41416-024-02740-5 Nat Commun, 2023, 14(1):4033
S8759	S55746	S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor (Ki = 1.3 nM) with poor affinity for BCL-XL and no significant binding to MCL-1, BFL-1 (BCL2A1/A1). The selectivity of S55746 for BCL-2 versus BCL-XL ranges from ~70 to 400 folds.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Signal Transduct Target Ther, 2022, 7(1):51
S5967	Berberine chloride hydrate	Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Biosci (Landmark Ed), 2022, 27(8):242 Front Pharmacol, 2021, 12:632201
E0124	Chelerythrine	Chelerythrine (Toddaline, Broussonpapyrine) is a potent, selective antagonist of PKC with an IC50 of 0.66 μM. Chelerythrine also inhibits the BclXL-Bak BH3 peptide binding with an IC50 of 1.5 μM. Chelerythrine shows antitumor, antidiabetic and anti-inflammatory activity.	Nutr Neurosci, 2022, 1-19
S3224	Cinobufagin	Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S6895	TCPOBOP	TCPOBOP is a constitutive androstane receptor (CAR) agonist. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
S9970	APG-2575 (lisaftoclax)	APG-2575 (lisaftoclax) is a dual Bcl-2 and Bcl-xl inhibitor with IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
S3243	Zeaxanthin	Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM.
E2354	Valepotriate	Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
E0011	Linderalactone	Linderalactone inhibits human lung cancer growth by modulating the expression of apoptosis-related proteins (Bax and Bcl-2) with an IC50 of 15 µM in A-549 cells. Linderalactone induces G2/M cell cycle arrest and could also suppress the JAK/STAT signalling pathway. Linderalactone can be isolated from Radix linderae.
E1510^New	Sonrotoclax	Sonrotoclax(BGB-11417) is a highly potent, orally active and selective inhibitor of Bcl2. Sonrotoclax demonstrates increased potency along with in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant. Bcl-xL Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712 J Biomol Struct Dyn, 2022, 1-11
S5600	Flavokawain A	Flavokawain A, extracted from kava, is an apoptotic inducers and anticarcinogenic agent. Flavokawain A can down-regulation of antiapoptotic proteins, such as XIAP, survivin, and Bcl-xL, thereby changing the balance between apoptotic and antiapoptotic molecules and then induce cell death in tumor cells.
S8177	BH3I-1	BH3I-1 is a Bcl-X_L-BH3 domain interaction inhibitor with Ki of 2.4 μM (by fluorescence polarization ).It is a selective inhibitor of Bcl-2 family proteins.
S8924	DT2216	DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
S6004	CCI-007	CCI-007 is a novel small molecule with cytotoxic activity against infant leukemia with MLL rearrangements.
S9665	Motixafortide (BL-8040)	Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ～1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.
S8758	VU661013	VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
S8550^New	AMG-176	AMG 176(Tapotoclax, Tapotoclaxum) is a potent, selective, and orally bioavailable macrocyclic inhibitor of MCL1 with a Ki of 0.13 nM. It induces a potent apoptosis in models of hematologic malignancies.
E2663	BT2	BT2 is a novel branched-chain α-ketoacid dehydrogenase complex kinase (BDK) inhibitor wieh an IC50 of 3.19 μM.
E3020	Hedyotic Diffusa Extract	Hedyotic Diffusa Extract is extracted from Hedyotic diffusa, of which polysaccharides inhibit the growth of CNE2 cells in a dose-and-time-dependent way, the mechanism may involve induction of cell apoptosis, which is associated with the activation of Bax and caspase-3 protein and the down-regulation of Bcl-2 protein expression.
S7747	Ro-3306	RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.	Nat Commun, 2024, 15(1):2089 Nucleic Acids Res, 2024, gkae747 Nucleic Acids Res, 2024, gkae263
S8650	BTSA1	BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.	bioRxiv, 2024, 10.1101/2023.01.18.524628 Cell Mol Life Sci, 2023, 80(10):311 Cell Mol Life Sci, 2023, 80(10):311
S7105	BAM7	BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.	Nat Chem Biol, 2019, 15(4):322-330 Cell Death Discov, 2018, 4:107
S3275	Senkyunolide I	Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	World J Emerg Med, 2024, 15(3):206-213 SSRN , 2024, 10.2139/ssrn.4696834 Cancer Biol Med, 2022, 19(11)j.issn.2095-3941.2022.0451
S3238	Resibufogenin	Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.	Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S9276	Alisol B	Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S5550	Ethyl gallate	Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. Ethyl gallat activates the death receptor-dependent pathway of apoptosis by enhancing the expression of caspases-8, -9, and -3 and the Bcl-2 interacting domain (Bid).
S6990	Phytohemagglutinin (PHA)	Phytohemagglutinin (PHA) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.	Molecules, 2023, 28(6)2426
S1057	Obatoclax Mesylate (GX15-070)	Obatoclax Mesylate (GX15-070) is an antagonist of Bcl-2 with K_i of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.	bioRxiv, 2024, 10.1101/2023.01.18.524628 Emerg Microbes Infect, 2022, 1-29 Cancers (Basel), 2022, 14(22)5602
S7100	WEHI-539	WEHI-539 has high affinity (IC50=1.1 nM) and selectivity for BCL-XL and potently kills cells by selectively antagonizing its prosurvival activity. It has more than a 400-fold higher affinity for BCL-XL versus other prosurvival BCL-2 family members.	Cell Rep Med, 2023, 4(11):101290 Liver Int, 2022, 10.1111/liv.15392 Cell Death Differ, 2021, 10.1038/s41418-021-00816-w
S6709	Obatoclax (GX15-070)	Obatoclax (GX15-070) is an antagonist of Bcl-2 with an Ki of 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis.	Oncotarget, 2024, 15:614-633 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
S7126	Marinopyrrole A (Maritoclax)	Marinopyrrole A (Maritoclax) is a selective Mcl-1 antagonist. It binds to Mcl-1, but not Bcl-XL, and targets Mcl-1 for proteasomal degradation. Maritoclax disrupts the interaction between Bim and Mcl-1 with an IC50 of 10.1 μM.	Clin Cancer Res, 2023, 29(2):446-457 Clin Cancer Res, 2023, 29(2):446-457 Cell Signal, 2022, S0898-6568(22)00041-9
S7849	BDA-366	BDA-366 is a small-molecule Bcl2-BH4 domain antagonist and binds BH4 with high affinity and selectivity. It directly binds to Bcl2 with high binding affinity (Ki =3.3 ± 0.73 nM).	BMC Cancer, 2023, 23(1):479
S8199	Ruxotemitide (LTX 315)	Ruxotemitide (LTX 315) is the oncolytic peptide that kills cancer cells through Bax/Bak-regulated mitochondrial membrane permeabilization.	J Immunother Cancer, 2022, 10(3)e004129 Nat Metab, 2021, 10.1038/s42255-021-00491-8
S0563	10-Deacetyl-7-xylosyl paclitaxel	10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.	Cell Death Dis, 2022, 13-9:799
S3245	Nodakenetin	Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity.
S3267	Nicotiflorin (Kaempferol-3-O-rutinoside)	Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
E2028	Humanin	Humanin (human) (1-24-Protein humanin (human)), a small mitochondrial-derived cytoprotective polypeptide encoded by mtDNA, exhibits protective effects in several cell types against cellular stress conditions and apoptosis through regulating various signaling mechanisms, such as JAK/STAT pathway and interaction of BCL-2 family of protein.
E1510^New	Sonrotoclax	Sonrotoclax(BGB-11417) is a highly potent, orally active and selective inhibitor of Bcl2. Sonrotoclax demonstrates increased potency along with in vitro and in vivo inhibitory activity against both WT Bcl-2 and the G101V mutant. Bcl-xL Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.
S8550^New	AMG-176	AMG 176(Tapotoclax, Tapotoclaxum) is a potent, selective, and orally bioavailable macrocyclic inhibitor of MCL1 with a Ki of 0.13 nM. It induces a potent apoptosis in models of hematologic malignancies.

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