p38α

p38α inhibitor 3 is a inhibitor of the mitogen-activated protein kinase p38α that can block the effectiveness of myoblast differentiation.

SD-169 (SD 169) is a selective and ATP competitive the MAP kinases p38α and p38β inhibitor.

SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.

Doramapimod (BIRB 796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.

AL 8697 is a selective p38α MAPK inhibitor (IC50 = 6 nM) with 14-fold selectivity over p38β (IC50 = 82 nM) and 300-fold selectivity over a panel of 91 kinases. AL 8697 has anti-inflammatory activity.

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

SR-318 is a potent and highly selective inhibitor of p38 MAPK, demonstrating IC50 values of 5 nM for p38α, 32 nM for p38β, and 6.11 μM for p38α/β. It possesses both anti-cancer and anti-inflammatory activity.

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

p38α inhibitor 4 is a selective MAPK p38α inhibitor, which is used to study diabetes, pain and chronic inflammation.

ARRY-797 (ARRY-371797) is a potent and selective p38α inhibitor and inhibits LPS-Induced IL-6.

The BMS-582949 hydrochloride (BMS-582949 HCl) is a highly specific p38α MAPK inhibitor (IC50: 13 nM).

AMG-548 is a selective and orally active p38α MAPK inhibitor (Ki = 0.5 nM), with higher selectivity than p38β, p38γ, and p38δ, and can also inhibit the TNFα, CK1δ/ε, and Wnt signalling pathways.

Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

SU3327 (halicin) is a potent, selective and substrate-competitive inhibitor of JNK(IC50 of 0.7 μM).

PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 is an effective inhibitor of inhaled p38 MAPK. PF-03715455 displays some selectivity for p38α over p38β (respective IC50: 0.88 and 23 nM). PF-0371545

RWJ-67657 (JNJ 3026582) is an orally active, selective p38α and p38β MAPK inhibitor (IC50s: 1 and 11 μM, respectively), with no activity at p38γ and p38δ, and demonstrates cardioprotective effects.

SJFα (SJF alpha) is a PROTAC formed by an E3 ubiquitin ligase-conjugated protein hydrolysis regulator that degrades p38α and p38δ and can be used in cancer research.

PH-797804 is a pyridinone inhibitor of p38α (IC50: 26 nM, in a cell-free assay); 4-fold more selective versus p38β and does not inhibit JNK2.

The compound p38α inhibitor5 (compound 1) is a PROTAC-type ligand that targets p38 and is utilized in the synthesis of NR-11c.

p38α-MK2-IN-1 (Compound 36) is an inhibitor of the p38α-MK2 complex, with an IC50 of 5 nM. This compound exhibits significant anti-inflammatory properties and has the ability to aid in joint repair.

p38α inhibitor8 (Compound 1) demonstrates inhibitory activity against p38αMAPK and CK1δ, with IC50 values of 0.21 µM and 0.202 µM, respectively.

p38α inhibitor9 (Compound 2015) is a p38α inhibitor that effectively blocks the enzyme activity of p38α, with an IC50 of less than 20 nM. It inhibits MK2T334 phosphorylation and activates Cdc25b and Cdc25c while inactivating Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy, and DNA damage. Additionally, p38α inhibitor9 can suppress colorectal cancer (CRC) metastasis.

p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.

SC-514 (GK 01140) is a selective, orally active, ATP-competitive IKK-2 inhibitor (IC50=11.2±4.7 μM), obstructs NF-κB-dependent gene expression.