p38β

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.

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.

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.

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.

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.

Losmapimod (GSK-AHAB) (GW856553X; SB856553; GSK-AHAB) is a specific, potent, and orally active p38 MAPK inhibitor (pKi: 8.1/7.6 for p38α/β).

UM-164 (DAS-DFGO-II), a highly potent c-Src inhibitor with a dissociation constant (Kd) of 2.7 nM, also effectively inhibits p38α and p38β.

Neflamapimod (VX-745) , a specific and effective inhibitor of p38α(IC50=10 nM), is 22-fold greater specificity against p38β and no inhibition activity to p38γ.

TAK-715 is a p38 MAPK inhibitor for p38α.

Pamapimod (R1503) (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 p38 gamma isoforms.

SB 239063 (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.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

EM 163 is a TIR-TIR interaction inhibitor, which is a TIR (Toll/interleukin-1 receptor) structural domain mimic of the MyD88 protein. EM 163 targets the TIR structural domain in the IL-1 receptor and blocks the interaction with MyD88. EM 163 inhibits the production of inflammatory cytokines in vivo caused by staphylococcal enterotoxin B (SEB). EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocked the activation of p38 and the inhibitory effect of IL-1β on chemically induced long-term potentiation (LTP)-triggered protein synthesis.

Methacycline hydrochloride (Rondomycin) is a broad-spectrum semisynthetic antibiotic related to TETRACYCLINE but excreted more slowly and maintaining effective blood levels for a more extended period.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK/p38 MAPK signaling pathways in the murine macrophages.

Chromium picolinate causes DNA damage and mutation. It is an activator of p38.

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. Isolated from hyssop oil, it possesses antifungal, highly active whitening, and antioxidant properties, and it has potential applications in cosmeceutical materials. It downregulates proinflammatory cytokines in vitro and in vivo, reduces the number of total cells, neutrophils, and macrophages in BALF, attenuates histologic lung alterations, decreases the wet-to-dry weight ratio in BALF, and inhibits the activation of NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, and p38 mitogen-activated protein kinase.

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

PP58 is an inhibitor of PDGFR, FGFR and Src family.