S1460 |
SP600125
|
SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
-
Cancer Cell, 2024, 42(4):535-551.e8
-
Nat Commun, 2024, 15(1):2581
-
Nat Commun, 2024, 15(1):987
|
|
S1574 |
Doramapimod (BIRB 796)
|
Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. |
-
J Immunother Cancer, 2024, 12(6)e009082
-
Aging Cell, 2024, e14093.
-
EMBO Rep, 2024, 10.1038/s44319-024-00149-y
|
|
S1950 |
Metformin HCl
|
Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
-
Nat Commun, 2024, 15(1):1785
-
J Clin Invest, 2024, e175023
-
EBioMedicine, 2024, 102:105090
|
|
S4901 |
JNK-IN-8
|
JNK-IN-8 (JNK Inhibitor XVI) is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line. |
-
Cell, 2024, 187(14):3652-3670.e40
-
Cancer Cell, 2024, 42(4):535-551.e8
-
Sci Rep, 2024, 14(1):11174
|
|
S7409 |
Anisomycin
|
Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis. |
-
Theranostics, 2024, 14(4):1561-1582
-
Research (Wash D C), 2024, 7:0331
-
Acta Biomater, 2024, S1742-7061(24)00036-9
|
|
S1396 |
Resveratrol
|
Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
-
Biochem Biophys Res Commun, 2024, 723:150186
-
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
-
Cell Death Dis, 2023, 14(6):367
|
|
S5958 |
Metformin
|
Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
-
Adv Healthc Mater, 2024, e2303785.
-
Cell Rep, 2024, 43(10):114775
-
J Transl Med, 2024, 22(1):723
|
|
S7508 |
JNK Inhibitor IX
|
JNK inhibitor IX (TCS JNK 5a) is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively. |
-
Cell Mol Immunol, 2023, 20(8):908-923
-
Nat Commun, 2023, 14(1):3364
-
Nat Commun, 2020, 11(1):258
|
|
S8490 |
Tanzisertib(CC-930)
|
Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. |
-
Cancer Cell, 2024, 42(4):535-551.e8
-
Signal Transduct Target Ther, 2023, 8(1):94
-
Viruses, 2023, 15(5)1112
|
|
S3901 |
Astragaloside IV
|
Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2. |
-
Cell Transplant, 2023, 32:9636897231198167
-
Cell Transplant, 2023, 32:9636897231198167
-
Cell Cycle, 2022, 1-14
|
|
S7794 |
JNK Inhibitor VIII
|
JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. |
-
Cell, 2024, 187(14):3652-3670.e40
-
Cell Death Discov, 2022, 8(1):113
-
Molecules, 2021, 26(8)2141
|
|
S8867 |
Bentamapimod (AS602801)
|
Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively. |
-
Front Oncol, 2022, 12:1006131
-
Front Oncol, 2022, 12:1006131
-
Nat Biomed Eng, 2018, 2(8):578-588
|
|
S3292 |
Falcarindiol
|
Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. |
-
Front Cell Infect Microbiol, 2023, 13:1128000
-
Front Pharmacol, 2021, 12:656697
|
|
S8201 |
BI-78D3
|
BI-78D3 is a competitive JNK inhibitor with IC50 of 280 nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. |
-
Neoplasia, 2021, 23(7):718-730
-
Cell Discov, 2019, 5:2
|
|
E1391 |
SP 600125, negative control
|
SP 600125, negative control (JNK inhibitor II, negative control) is a methylated analog of SP 600125 and inhibits JNK2 and JNK3 with IC50 of 18 µM and 24 µM, respectively. |
-
Cell Death Dis, 2023, 14(8):537
|
|
S7637 |
DTP3
|
DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway. |
-
Life Sci Alliance, 2024, 7(8)e202302555
-
MedComm (2020), 2023, 4(3):e269
|
|
S6730 |
CC-401 Hydrochloride
|
CC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases. |
-
Insect Biochem Mol Biol, 2016, 73:55-61
|
|
S3811 |
Ginsenoside Re
|
Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
-
J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S9114 |
Polyphyllin I
|
Polyphyllin I, a small molecular monomer extracted from Rhizoma of Paris polyphyllin, is used in the treatment of infectious disease and cancer. Polyphyllin I inhibits proliferation and induces apoptotic cell death in U251 cells. Polyphyllin I is an activator of the JNK signaling pathway with a potential anti-glioma effect. |
-
Mol Med, 2024, 30(1):59
-
Oxid Med Cell Longev, 2022, 2022:4031008
|
|
S6740 |
DB07268
|
DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK. |
|
|
S3940 |
3'-Hydroxypterostilbene
|
3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways. |
|
|
S4643 |
KB-R7943 mesylate
|
KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux. |
|
|
E2653 |
JNK-IN-7
|
JNK-IN-7 is a strong JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, which inhibits phosphorylation of c-Jun, direct substrate of JNK kinase. |
|
|
S3242 |
Loureirin B
|
Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular. |
|
|
S0949 |
Cucurbitacin IIb
|
Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis. |
|
|
S4884 |
Trans-Zeatin
|
Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently. |
|
|
S9614New |
CC-90001
|
CC-90001 is an orally administered inhibitor of c-Jun N-terminal kinase (JNK) with bias for JNK1 over JNK2. It exhibits antifibrotic efficacy and can be used for the research of idiopathic pulmonary fibrosis. |
|
|
S9698 |
Ezatiostat
|
Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis. |
|
|
S0781 |
IQ 3
|
IQ 3 is a specific c-Jun N-terminal kinase (JNK) inhibitor with Kd of 66 nM, 240 nM and 290 nM for JNK3, JNK1 and JNK2, respectively. IQ 3 inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. IQ 3 also inhibits TNF-α and IL-6 production in vitro. |
-
Int J Biol Sci, 2024, 20(6):2323-2338
|
|
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
|
|
E2252 |
SU3327
|
SU3327 is a potent, selective and substrate-competitive c-Jun N-terminal kinase (JNK) inhibitor with an IC50 of 0.7 μM. |
|
|
E1656 |
AS601245
|
AS601245 is an orally active, selective, ATP-competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50 of 150, 220, and 70 nM for three JNK human isoforms hJNK1, hJNK2, and hJNK3, respectively. |
|
|
E3640 |
Dendrobii caulis Extract
|
Dendrobii Caulis Extract is extracted from Dendrobii Caulis, which can protect fibroblasts against UVA-induced photoaging via JNK/c-Jun/MMPs pathway. |
|
|
E0072 |
Indirubin-3′-oxime
|
Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
|
|
|
S0844 |
NDMC101
|
NDMC101 inhibits osteoclastogenesis which also ameliorates paw swelling and inflammatory bone destruction, associating with the inhibition of such transcription factors as NF-κB and NFATc1 as well as multiple protein kinases, including p38, ERK, and JNK. |
|
|
S9075 |
Mulberroside A
|
Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38. |
|
|
E2682 |
RPI-1
|
RPI-1 inhibits proliferation of human papillary thyroid carcinoma cell line TPC-1 by inducing accumulation of cells at the G2 cell cycle phase, abolishes Ret/Ptc1 tyrosine phosphorylation along with its binding to Shc and phospholipase Cg, also abolishes the activation of JNK2 and AKT. |
|
|
S4460 |
IMM-H007
|
IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux. |
|
|
S6347 |
5'-N-Ethylcarboxamidoadenosine (NECA)
|
5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway. |
|
|
S6711 |
IQ-1S
|
IQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively. |
|
|
S1321 |
Urolithin B
|
Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. |
|
|
S1460 |
SP600125
|
SP600125 (Nsc75890) is a broad-spectrum JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 40 nM, 40 nM and 90 nM in cell-free assays, respectively; 10-fold greater selectivity against MKK4, 25-fold greater selectivity against MKK3, MKK6, PKB, and PKCα, and 100-fold selectivity against ERK2, p38, Chk1, EGFR etc. SP600125 is also a broad‐spectrum inhibitor of serine/threonine kinases including Aurora kinase A,FLT3 and TRKA with of IC50 of 60 nM, 90 nM and 70 nM. SP600125 inhibits autophagy and activates apoptosis. |
- Cancer Cell, 2024, 42(4):535-551.e8
- Nat Commun, 2024, 15(1):2581
- Nat Commun, 2024, 15(1):987
|
|
S1574 |
Doramapimod (BIRB 796)
|
Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2. |
- J Immunother Cancer, 2024, 12(6)e009082
- Aging Cell, 2024, e14093.
- EMBO Rep, 2024, 10.1038/s44319-024-00149-y
|
|
S4901 |
JNK-IN-8
|
JNK-IN-8 (JNK Inhibitor XVI) is the first irreversible JNK inhibitor for JNK1, JNK2 and JNK3 with IC50 of 4.7 nM, 18.7 nM and 1 nM, >10-fold selectivity against MNK2, Fms and no inhibition to c-Kit, Met, PDGFRβin A375 cell line. |
- Cell, 2024, 187(14):3652-3670.e40
- Cancer Cell, 2024, 42(4):535-551.e8
- Sci Rep, 2024, 14(1):11174
|
|
S1396 |
Resveratrol
|
Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis. |
- Biochem Biophys Res Commun, 2024, 723:150186
- J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
- Cell Death Dis, 2023, 14(6):367
|
|
S7508 |
JNK Inhibitor IX
|
JNK inhibitor IX (TCS JNK 5a) is a selective and potent JNK inhibitor with pIC50 of 6.5 and 6.7 for JNK2 and JNK3, respectively. |
- Cell Mol Immunol, 2023, 20(8):908-923
- Nat Commun, 2023, 14(1):3364
- Nat Commun, 2020, 11(1):258
|
|
S8490 |
Tanzisertib(CC-930)
|
Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK-dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively. |
- Cancer Cell, 2024, 42(4):535-551.e8
- Signal Transduct Target Ther, 2023, 8(1):94
- Viruses, 2023, 15(5)1112
|
|
S3901 |
Astragaloside IV
|
Astragaloside IV (AST-IV, AS-IV) is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine. It has various effect on the cardiovascular, immune, digestive, and nervous systems. AS-IV suppresses activation of p-Akt, p-mTOR, p-NF-κB and p-Erk1/2. |
- Cell Transplant, 2023, 32:9636897231198167
- Cell Transplant, 2023, 32:9636897231198167
- Cell Cycle, 2022, 1-14
|
|
S7794 |
JNK Inhibitor VIII
|
JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively. |
- Cell, 2024, 187(14):3652-3670.e40
- Cell Death Discov, 2022, 8(1):113
- Molecules, 2021, 26(8)2141
|
|
S8867 |
Bentamapimod (AS602801)
|
Bentamapimod (AS602801) is a novel, orally active JNK inhibitor with IC50 values of 80 nM, 90 nM and 230 nM for JNK1, JNK2 and JNK3 respectively. |
- Front Oncol, 2022, 12:1006131
- Front Oncol, 2022, 12:1006131
- Nat Biomed Eng, 2018, 2(8):578-588
|
|
S3292 |
Falcarindiol
|
Falcarindiol (FAD, (3R,8S)-Falcarindiol, FaDOH) is a natural polyacetylene compound found rich in many plants of the Umbelliferae family. Falcarindiol suppresses LPS-stimulated expression of inducible nitric oxide synthase (iNOS), tumor necrosis factor alpha (TNFα), interleukin-6 (IL-6), and interleukin-1 beta (IL-1β). Falcarindiol attenuates the LPS-induced activation of JNK, ERK, STAT1, and STAT3 signaling molecules. |
- Front Cell Infect Microbiol, 2023, 13:1128000
- Front Pharmacol, 2021, 12:656697
|
|
S8201 |
BI-78D3
|
BI-78D3 is a competitive JNK inhibitor with IC50 of 280 nM that displays > 100 fold selectivity over p38α and no activity at mTOR and PI-3K. |
- Neoplasia, 2021, 23(7):718-730
- Cell Discov, 2019, 5:2
|
|
E1391 |
SP 600125, negative control
|
SP 600125, negative control (JNK inhibitor II, negative control) is a methylated analog of SP 600125 and inhibits JNK2 and JNK3 with IC50 of 18 µM and 24 µM, respectively. |
- Cell Death Dis, 2023, 14(8):537
|
|
S6730 |
CC-401 Hydrochloride
|
CC-401 is a potent inhibitor of JNK with at least 40-fold selectivity against other related kinases. |
- Insect Biochem Mol Biol, 2016, 73:55-61
|
|
S3811 |
Ginsenoside Re
|
Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB. |
- J Ethnopharmacol, 2021, S0378-8741(21)00169-0
|
|
S6740 |
DB07268
|
DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK. |
|
|
E2653 |
JNK-IN-7
|
JNK-IN-7 is a strong JNK inhibitor with IC50 of 1.5, 2 and 0.7 nM for JNK1, JNK2 and JNK3, which inhibits phosphorylation of c-Jun, direct substrate of JNK kinase. |
|
|
S3242 |
Loureirin B
|
Loureirin B (LB, LrB), a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of PAI-1 with IC50 of 26.10 μM. Loureirin B downregulates p-ERK and p-JNK in TGF-β1-stimulated fibroblasts. Loureirin B promotes insulin secretion mainly through increasing Pdx-1, MafA, intracellular ATP level, inhibiting the KATP current, influx of Ca2+ to the intracellular. |
|
|
S0949 |
Cucurbitacin IIb
|
Cucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis. |
|
|
S4884 |
Trans-Zeatin
|
Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently. |
|
|
S9614New |
CC-90001
|
CC-90001 is an orally administered inhibitor of c-Jun N-terminal kinase (JNK) with bias for JNK1 over JNK2. It exhibits antifibrotic efficacy and can be used for the research of idiopathic pulmonary fibrosis. |
|
|
S0781 |
IQ 3
|
IQ 3 is a specific c-Jun N-terminal kinase (JNK) inhibitor with Kd of 66 nM, 240 nM and 290 nM for JNK3, JNK1 and JNK2, respectively. IQ 3 inhibits LPS-induced NF-κB/AP1 transcriptional activity in THP1-Blue cells with IC50 of 1.4 μM. IQ 3 also inhibits TNF-α and IL-6 production in vitro. |
- Int J Biol Sci, 2024, 20(6):2323-2338
|
|
E2252 |
SU3327
|
SU3327 is a potent, selective and substrate-competitive c-Jun N-terminal kinase (JNK) inhibitor with an IC50 of 0.7 μM. |
|
|
E1656 |
AS601245
|
AS601245 is an orally active, selective, ATP-competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50 of 150, 220, and 70 nM for three JNK human isoforms hJNK1, hJNK2, and hJNK3, respectively. |
|
|
E3640 |
Dendrobii caulis Extract
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Dendrobii Caulis Extract is extracted from Dendrobii Caulis, which can protect fibroblasts against UVA-induced photoaging via JNK/c-Jun/MMPs pathway. |
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E0072 |
Indirubin-3′-oxime
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Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity.
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S9075 |
Mulberroside A
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Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38. |
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E2682 |
RPI-1
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RPI-1 inhibits proliferation of human papillary thyroid carcinoma cell line TPC-1 by inducing accumulation of cells at the G2 cell cycle phase, abolishes Ret/Ptc1 tyrosine phosphorylation along with its binding to Shc and phospholipase Cg, also abolishes the activation of JNK2 and AKT. |
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S4460 |
IMM-H007
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IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux. |
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S6347 |
5'-N-Ethylcarboxamidoadenosine (NECA)
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5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway. |
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S6711 |
IQ-1S
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IQ-1S is a JNK3 inhibitor with Kd values of 87, 360 and 390 nM for JNK3, JNK2 and JNK1, respectively. |
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S1321 |
Urolithin B
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Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. |
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S1950 |
Metformin HCl
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Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
- Nat Commun, 2024, 15(1):1785
- J Clin Invest, 2024, e175023
- EBioMedicine, 2024, 102:105090
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S7409 |
Anisomycin
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Anisomycin (Flagecidin, Wuningmeisu C) is a bacterial antibiotic isolated from Streptomyces griseolus, which inhibits protein synthesis, and also act as a JNK activator. Anisomycin upregulates autophagy and increases apoptosis. |
- Theranostics, 2024, 14(4):1561-1582
- Research (Wash D C), 2024, 7:0331
- Acta Biomater, 2024, S1742-7061(24)00036-9
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S5958 |
Metformin
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Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
- Adv Healthc Mater, 2024, e2303785.
- Cell Rep, 2024, 43(10):114775
- J Transl Med, 2024, 22(1):723
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S7637 |
DTP3
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DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. DTP3 inhibits cancer-selective NF-κB survival pathway. |
- Life Sci Alliance, 2024, 7(8)e202302555
- MedComm (2020), 2023, 4(3):e269
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S9114 |
Polyphyllin I
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Polyphyllin I, a small molecular monomer extracted from Rhizoma of Paris polyphyllin, is used in the treatment of infectious disease and cancer. Polyphyllin I inhibits proliferation and induces apoptotic cell death in U251 cells. Polyphyllin I is an activator of the JNK signaling pathway with a potential anti-glioma effect. |
- Mol Med, 2024, 30(1):59
- Oxid Med Cell Longev, 2022, 2022:4031008
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S3940 |
3'-Hydroxypterostilbene
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3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways. |
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S4643 |
KB-R7943 mesylate
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KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM. KB-R7943 mesylate promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux. |
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S9698 |
Ezatiostat
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Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis. |
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S2271 |
Berberine chloride
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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
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