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p38 MAPK Signaling Pathway

p38 MAPK Products

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  • New p38 MAPK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1076 Adezmapimod (SB203580) Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.
Nat Commun, 2024, 15(1):987
Nat Commun, 2024, 15(1):1300
Acta Pharm Sin B, 2024, 14(4):1693-1710
S1077 SB202190 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):5874
Nat Commun, 2024, 15(1):4124
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
S1494 Ralimetinib (LY2228820) dimesylate Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
Immunity, 2024, 57(7):1514-1532.e15
Cell Death Dis, 2024, 15(4):273
J Cell Physiol, 2024, 10.1002/jcp.31172
S2726 PH-797804 PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
Signal Transduct Target Ther, 2024, 9(1):39
Cell Signal, 2024, 114:111004
BMC Cancer, 2024, 24(1):520
S6005 VX-702 VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
Immunology, 2024, 10.1111/imm.13773
Nat Commun, 2023, 14(1):861
Antiviral Res, 2022, 209:105475
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
S7686 ML141 ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
J Nanobiotechnology, 2024, 22(1):357
Genes Cancer, 2024, 15:15-27
Exp Mol Med, 2023, 55(4):779-793
S7215 Losmapimod Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):987
Int J Mol Sci, 2024, 25(13)7302
J Radiat Res, 2024, rrae021
S7741 SB239063 SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
Cancers (Basel), 2023, 15(3)961
Cancers (Basel), 2023, 15(3)961
J Pain, 2023, S1526-5900(23)00013-5
S1458 Neflamapimod (VX-745) Neflamapimod (VX-745) is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.
Biology (Basel), 2022, 11(1)121
EMBO J, 2021, e106188
Cell, 2020, 182(3):685-712.e19
S8124 BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
Mol Med Rep, 2023, 27(2)47
EMBO J, 2021, e107182
Cell, 2020, 182(3):685-712.e19
S7214 Skepinone-L Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
J Biol Chem, 2023, S0021-9258(23)00341-1
Nat Neurosci, 2022, 25(9):1149-1162
Elife, 2022, 11e80953
S2266 Asiatic Acid Asiatic acid (Dammarolic acid, Asiantic acid) is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.
Front Pharmacol, 2023, 14:1264324
Gut Microbes, 2022, 14(1):2057779
Stem Cell Res Ther, 2022, 13(1):531
S2928 TAK-715 TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.
Life (Basel), 2023, 13(2)412
Life (Basel), 2023, 13(2)412
Chem Biol Interact, 2022, 363:110010
S8125 Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.
J Leukoc Biol, 2020, 10.1002/JLB.3A0120-379RR
J Pharmacol Exp Ther, 2020, 374(3):489-498
Nat Commun, 2019, 10(1):688
S7799 Pexmetinib Pexmetinib is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
J Bone Oncol, 2022, 35:100439
Theranostics, 2021, 11(4):1626-1640
Sci Rep, 2021, 11(1):5752
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
S6502 SD 0006 SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β).
Eur Rev Med Pharmacol Sci, 2020, 24(21):10966-10974
S0542 R1487 R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM.
Drug Test Anal, 2020, 10.1002/dta.2917
S8706 UM-164 UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
Cancers (Basel, 2022, 14(215343)
S5183 PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.
PLoS One, 2021, 16(5):e0252541
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.
S9514 Rotundic acid Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.
E2372 p38-α MAPK-IN-1 p38-α MAPK-IN-1 is an inhibitor of p38-α, with IC50 value of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
E3566 Largeleaf Gentian Root Extract Largeleaf Gentian Root Extract is extracted from the root of Gentiana macrophylla, which can modulate the CD147/p38/NF-κB pathway.
S8989 Xanthatin Xanthatin is a sesquiterpene lactone isolated from Xanthium strumarium leaves, which can inhibit the nuclear factor kappa-B (NF-κB), mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STATs) signaling pathways.
S0752 AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
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.
E3656 Dichroa febrifuga Extract Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
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
E3328 Suberect spatholobus stem Extract Suberect spatholobus stem Extract is extracted from Suberect spatholobus stem, which can Inhibiti TGF-β1/p38MAPK signaling pathway and the synthesis of ColⅠ, thereby playing a role in the treatment of liver fibrosis.
E0114 Dilmapimod (SB-681323) Dilmapimod (SB-681323,GW 681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.
S9315 Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
E3365 Weigela Grandiflora Fortune Extract Weigela Grandiflora Fortune Extract is extracted from Weigela Grandiflora Fortune, which decreases the infection-mediated expression of inflammatory mediators by inhibiting the AKT/NF-κB and MAPK signaling pathways.
S0387 SB 242235 SB-242235 is a potent and selective p38 MAP kinase inhibitor, inhibits p38 MAP kinase induced by IL-1β with an IC50 of approximately 1.0 μM in primary human chondrocytes.
S0388 SD169 SD-169(5-Carbamoylindole) is a selective inhibitor of p38α MAPK, which can reduce p38 and HSP60 expression in T cells of the pancreatic beta islets.
E3592 Panax notoginseng Root Extract Panax Notoginseng Root Extract is extracted from the root of Panax Notoginseng, which exerts protective effect on metabolic syndrome through MAPK-mediated adipose thermogenic activation.
E3593 Panax notoginseng Rhizoma Extract Panax Notoginseng Rhizoma Extract is extracted from the rhizoma of Panax Notoginseng, which exerts protective effect on metabolic syndrome through MAPK-mediated adipose thermogenic activation.
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.
S0186 TA-01 TA-01 is a potent inhibitor of CK1δ/ε and p38 MAPK with IC50 of 6.4 nM, 6.8 nM and 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
E0526 sappanone A Sappanone A, a homoisoflavanone isolated from the heartwood of Caesalpinia sappan (Leguminosae), induces HO-1 expression by activating Nrf2 through the p38 MAPK pathway, suppresses LPS-induced NF-κB activation by suppressing the phosphorylation of RelA/p65 at Ser536, exerting its anti-inflammatory effect.
E2399 Falnidamol Falnidamol (BIBX1382) is a selective inhibitor of epidermal growth factor receptor (EGFR), exerting anti-cancer role in human head and neck squamous cell carcinomas both in vitro and in vivo through suppressing mitogen-activated protein kinases (MAPKs) signaling.
E2630 SKF-86002 SKF-86002 is an orally active p38 MAPK inhibitor, inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production with IC50 of 1 μM, also inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
S3888 3,4',5-Trimethoxy-trans-stilbene 3,4',5-Trimethoxy-trans-stilbene (MR-3) is a methylated derivative of resveratrol and shows more potent inhibitory effects on the growth of human cancer cells (HT-29, PC-3, COLO 205) with IC50 values of 81.31, 42.71 and 6.25 μM, respectively.
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.
E2661 Chitosan oligosaccharide Chitosan oligosaccharide (COS) is an oligomer of β-(1➔4)-linked d-glucosamine, of which actions involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK).
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
E3786 Radix Scrophulariae Extract Radix Scrophulariae Extract is derived from Radix Scrophulariae, which has anti-apoptotic and anti-inflammatory effects, potentially operating by affecting the mitogen-activated protein kinases (MAPKs) signaling pathway and inhibition of the NF-κB pathway.
E3033 Pulsatillae Extract Pulsatillae Extract is extracted from Pulsatilla chinensis, major active constituent of which can reduce tumorigenesis, metastasis and immunosuppression of tumor via disruption of the MAPK signaling pathway.
S1076 Adezmapimod (SB203580) Adezmapimod (SB203580, RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.
Nat Commun, 2024, 15(1):987
Nat Commun, 2024, 15(1):1300
Acta Pharm Sin B, 2024, 14(4):1693-1710
S1077 SB202190 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Nat Commun, 2024, 15(1):4124
Nat Commun, 2024, 15(1):5874
Nat Commun, 2024, 15(1):4124
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
S1494 Ralimetinib (LY2228820) dimesylate Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
Immunity, 2024, 57(7):1514-1532.e15
Cell Death Dis, 2024, 15(4):273
J Cell Physiol, 2024, 10.1002/jcp.31172
S2726 PH-797804 PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
Signal Transduct Target Ther, 2024, 9(1):39
Cell Signal, 2024, 114:111004
BMC Cancer, 2024, 24(1):520
S6005 VX-702 VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
Immunology, 2024, 10.1111/imm.13773
Nat Commun, 2023, 14(1):861
Antiviral Res, 2022, 209:105475
S7215 Losmapimod Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.
Nat Commun, 2024, 15(1):987
Int J Mol Sci, 2024, 25(13)7302
J Radiat Res, 2024, rrae021
S7741 SB239063 SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
Cancers (Basel), 2023, 15(3)961
Cancers (Basel), 2023, 15(3)961
J Pain, 2023, S1526-5900(23)00013-5
S1458 Neflamapimod (VX-745) Neflamapimod (VX-745) is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.
Biology (Basel), 2022, 11(1)121
EMBO J, 2021, e106188
Cell, 2020, 182(3):685-712.e19
S8124 BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.
Mol Med Rep, 2023, 27(2)47
EMBO J, 2021, e107182
Cell, 2020, 182(3):685-712.e19
S7214 Skepinone-L Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
J Biol Chem, 2023, S0021-9258(23)00341-1
Nat Neurosci, 2022, 25(9):1149-1162
Elife, 2022, 11e80953
S2928 TAK-715 TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.
Life (Basel), 2023, 13(2)412
Life (Basel), 2023, 13(2)412
Chem Biol Interact, 2022, 363:110010
S8125 Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.
J Leukoc Biol, 2020, 10.1002/JLB.3A0120-379RR
J Pharmacol Exp Ther, 2020, 374(3):489-498
Nat Commun, 2019, 10(1):688
S7799 Pexmetinib Pexmetinib is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
J Bone Oncol, 2022, 35:100439
Theranostics, 2021, 11(4):1626-1640
Sci Rep, 2021, 11(1):5752
S6502 SD 0006 SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β).
Eur Rev Med Pharmacol Sci, 2020, 24(21):10966-10974
S0542 R1487 R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM.
Drug Test Anal, 2020, 10.1002/dta.2917
S8706 UM-164 UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
Cancers (Basel, 2022, 14(215343)
S5183 PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.
PLoS One, 2021, 16(5):e0252541
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.
E2372 p38-α MAPK-IN-1 p38-α MAPK-IN-1 is an inhibitor of p38-α, with IC50 value of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
S8989 Xanthatin Xanthatin is a sesquiterpene lactone isolated from Xanthium strumarium leaves, which can inhibit the nuclear factor kappa-B (NF-κB), mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STATs) signaling pathways.
S0752 AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
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.
E3656 Dichroa febrifuga Extract Dichroa Febrifuga Extract is extracted from Dichroa Febrifuga, which can Suppress PI3K/AKT and MAPK Signaling Pathways.
E3328 Suberect spatholobus stem Extract Suberect spatholobus stem Extract is extracted from Suberect spatholobus stem, which can Inhibiti TGF-β1/p38MAPK signaling pathway and the synthesis of ColⅠ, thereby playing a role in the treatment of liver fibrosis.
E0114 Dilmapimod (SB-681323) Dilmapimod (SB-681323,GW 681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.
S9315 Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
E3365 Weigela Grandiflora Fortune Extract Weigela Grandiflora Fortune Extract is extracted from Weigela Grandiflora Fortune, which decreases the infection-mediated expression of inflammatory mediators by inhibiting the AKT/NF-κB and MAPK signaling pathways.
S0387 SB 242235 SB-242235 is a potent and selective p38 MAP kinase inhibitor, inhibits p38 MAP kinase induced by IL-1β with an IC50 of approximately 1.0 μM in primary human chondrocytes.
S0388 SD169 SD-169(5-Carbamoylindole) is a selective inhibitor of p38α MAPK, which can reduce p38 and HSP60 expression in T cells of the pancreatic beta islets.
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.
S0186 TA-01 TA-01 is a potent inhibitor of CK1δ/ε and p38 MAPK with IC50 of 6.4 nM, 6.8 nM and 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively.
E2399 Falnidamol Falnidamol (BIBX1382) is a selective inhibitor of epidermal growth factor receptor (EGFR), exerting anti-cancer role in human head and neck squamous cell carcinomas both in vitro and in vivo through suppressing mitogen-activated protein kinases (MAPKs) signaling.
E2630 SKF-86002 SKF-86002 is an orally active p38 MAPK inhibitor, inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production with IC50 of 1 μM, also inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
S3888 3,4',5-Trimethoxy-trans-stilbene 3,4',5-Trimethoxy-trans-stilbene (MR-3) is a methylated derivative of resveratrol and shows more potent inhibitory effects on the growth of human cancer cells (HT-29, PC-3, COLO 205) with IC50 values of 81.31, 42.71 and 6.25 μM, respectively.
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.
E2661 Chitosan oligosaccharide Chitosan oligosaccharide (COS) is an oligomer of β-(1➔4)-linked d-glucosamine, of which actions involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK).
S6807 TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
E3033 Pulsatillae Extract Pulsatillae Extract is extracted from Pulsatilla chinensis, major active constituent of which can reduce tumorigenesis, metastasis and immunosuppression of tumor via disruption of the MAPK signaling pathway.
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
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
S7686 ML141 ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
J Nanobiotechnology, 2024, 22(1):357
Genes Cancer, 2024, 15:15-27
Exp Mol Med, 2023, 55(4):779-793
S2266 Asiatic Acid Asiatic acid (Dammarolic acid, Asiantic acid) is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.
Front Pharmacol, 2023, 14:1264324
Gut Microbes, 2022, 14(1):2057779
Stem Cell Res Ther, 2022, 13(1):531
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
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
E0526 sappanone A Sappanone A, a homoisoflavanone isolated from the heartwood of Caesalpinia sappan (Leguminosae), induces HO-1 expression by activating Nrf2 through the p38 MAPK pathway, suppresses LPS-induced NF-κB activation by suppressing the phosphorylation of RelA/p65 at Ser536, exerting its anti-inflammatory effect.
S9514 Rotundic acid Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.
E3566 Largeleaf Gentian Root Extract Largeleaf Gentian Root Extract is extracted from the root of Gentiana macrophylla, which can modulate the CD147/p38/NF-κB pathway.

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