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
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.
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.
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
S7214 Skepinone-L Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
  • Cell Physiol Biochem, 2015, 36(2):631-641
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.
S2266 Asiatic Acid Asiatic acid is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.

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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
S7741 SB239063 <1 mg/mL 60 mg/mL 7 mg/mL
S7799 Pexmetinib (ARRY-614) <1 mg/mL 100 mg/mL 100 mg/mL
S7215 Losmapimod (GW856553X) <1 mg/mL 76 mg/mL 41 mg/mL
S7214 Skepinone-L <1 mg/mL 85 mg/mL 85 mg/mL
S2928 TAK-715 <1 mg/mL 80 mg/mL 16 mg/mL
S2266 Asiatic Acid <1 mg/mL 97 mg/mL <1 mg/mL
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