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.

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.

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

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.

Ralimetinib dimesylate (LY2228820 dimesylate) is the dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities.

TAK-715 is a p38 MAPK inhibitor for p38α.

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

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 Inhibitor 2, a potent and selective inhibitor of p38α MAPK, exhibits a pIC50 value of 9.6. It also demonstrates inhibition of the hERG ion channel (IC50=27 μM) and maintains promising selectivity, with <30% inhibition across a panel of 51 protein kinases at a 10 μM concentration and a broad specificity against 141 other biological targets[1].

WYE-687 is an ATP-competitive and selective inhibitor of mTOR with an IC50 of 7 nM; it blocks mTORC1 pS6K(T389) and mTORC2 P-AKT(S473) without affecting P-AKT(T308). Its selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

ERK2 p38α MAPK-IN-1 (Compound 1, In silico Hit-2), a selective inhibitor of ERK2 and p38α MAPK, exhibits potent activity with an IC 50 of 82 μM against ERK2. It uniquely binds to the allosteric sites of both ERK2 and p38α MAPK. This compound is utilized for type 2 diabetes research [1].

p38αMAPK CK1δ inhibitor-1 (Compound 3) exhibits inhibitory activity against p38αMAPK and CK1δ, with IC50 values of 0.185 µM and 0.089 µM, respectively.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

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.

Bongkrekic acid (Bongkrekic Acid (ammonium salt)) is a mitochondrial toxin secreted by Burkholderia gladioli that inhibits adenine nucleotide translocase (ANT).Bongkrekic acid Bongkrekic acid Bongkrekic acid induces extracellular traps in neutrophils through signaling mediated by p38, ERK, PAD4, and P2X1.

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK p38 MAPK pathways.

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, effectively inhibiting BRAF (WT), BRAF (V600E), and wild-type CRAF [IC50s: 79 38 68 nM].

1. Isofraxidin (Phytodolor) protects leukemia cells from radiation-induced apoptosis via ROS mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS-induced ALI, and the protective effect of Isofraxidin seems to result from the inhibition of COX-2 protein expression in the lung, which regulates the production of PGE2. 3. Isofraxidin possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1 2.