p38 MAPK

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p38 MAPK Inhibitors | Activators (13)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1076 SB203580 SB203580 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.
  • J Exp Med, 2015, 212(4):525-38
  • Hepatology, 2014, 59(4):1262-72
  • Leukemia, 2014, 28(10):2109-12
S1574 BIRB 796 (Doramapimod) BIRB 796 (Doramapimod) 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.
  • Mol Syst Biol, 2015, 11(3):797
  • J Exp Med, 2015, 212(4):525-38
  • Blood, 2012, 119(26):6255-8
S1077 SB202190 (FHPI) SB202190 (FHPI) 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.
  • Mol Syst Biol, 2015, 11(3):797
  • Nat Commun, 2014, 5:3479
  • Clin Cancer Res, 2016, 10.1158/1078-0432.CCR-15-2242
S1494 LY2228820 LY2228820 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.
  • Cancer Cell, 2016, 10.1016/j.ccell.2016.01.006
  • J Exp Med, 2015, 212(4):525-38
  • Blood, 2012, 119(26):6255-8
S6005 VX-702 VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
  • Autophagy, 2016, 12(2):432-8
  • Stem Cell Reports, 2014, 3(1):34-43
  • PLoS One, 2013, 8(8): e70732
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.
  • Nat Cell Biol, 2014, 16(7):685-94
  • EMBO Mol Med, 2014, 5(11):1759-74
  • Oncotarget, 2014, 5(10):3145-58
S1458 VX-745 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.
  • Mol Cell Proteomics, 2012, 11(6):M112.017764
  • Br J Pharmacol, 2012, 166(3):858-76
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.
S7214 Skepinone-L Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
  • Cell Physiol Biochem, 2015, 36(2):631-641
S2266 Asiatic Acid Asiatic acid is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S7215 Losmapimod (GW856553X) Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
  • Auton Autacoid Pharmacol, 2015, 35(3):32-40
S7799 Pexmetinib (ARRY-614) Pexmetinib (ARRY-614) 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.
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.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1076 SB203580 <1 mg/mL 43 mg/mL <1 mg/mL
S1574 BIRB 796 (Doramapimod) <1 mg/mL 106 mg/mL 106 mg/mL
S1077 SB202190 (FHPI) <1 mg/mL 66 mg/mL 12 mg/mL
S1494 LY2228820 100 mg/mL 4 mg/mL 3 mg/mL
S6005 VX-702 <1 mg/mL 81 mg/mL <1 mg/mL
S2726 PH-797804 <1 mg/mL 96 mg/mL 7 mg/mL
S1458 VX-745 <1 mg/mL 15 mg/mL <1 mg/mL
S2928 TAK-715 <1 mg/mL 80 mg/mL 16 mg/mL
S7214 Skepinone-L <1 mg/mL 85 mg/mL 85 mg/mL
S2266 Asiatic Acid <1 mg/mL 97 mg/mL <1 mg/mL
S7215 Losmapimod (GW856553X) <1 mg/mL 76 mg/mL 41 mg/mL
S7799 Pexmetinib (ARRY-614) <1 mg/mL 100 mg/mL 100 mg/mL
S7741 SB239063 <1 mg/mL 60 mg/mL 7 mg/mL
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