active protein kinase

GSK-1520489A is an active PKMYT1 inhibitor.

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.

LP-922761 is a potent, selective, and orally active AAK1 inhibitor with inhibitory effects on BMP-2 induced protein kinase (BIKE).

UR-13870 (Org 48762-0) is an orally active and selective inhibitor of p38 mitogen-activated protein kinase (MAPK), which prevents bone damage in collagen-induced arthritis in mice.

Emprumapimod (PF-07265803) is an orally active and specific inhibitor of mitogen-activated protein kinase p38α MAPK, inhibits LPS-induced production of IL-6, and can be used to study dilated cardiomyopathy induced by the LMNA gene.

TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1].

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

(-)-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.

Pim-1/2 Kinase Inhibitor 1, an orally active inhibitor, impedes the action of Pim kinases by preventing their ability to phosphorylate peptides. It particularly inhibits the phosphorylation of 4E-BP1 and p27 Kip1 by Pim protein kinases. This compound is valuable in cancer research, with a notable application in studying prostate cancer [1].

ZIP acetate is a novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-ph

BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.

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

Bufalin is a natural product and a Na⁺/K⁺-ATPase inhibitor (IC50 ≈ 40–45 nM) with favorable cell permeability. By binding to α subunits such as ATP1A1, bufalin induces calcium overload and pyroptosis, and can be used for experimental research and therapeutic exploration in various cancers.

Purine riboside-5'-O-triphosphate sodium is an active metabolite of Nebularine and acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC50 values of 35 µM and 28 µM, respectively. It also inhibits calmodulin-dependent protein kinase II (CaMKII), with a Ki value of 590 µM.

HW161023 (compound) is an orally active inhibitor of AP2 associated protein kinase 1 (AAK1), exhibiting IC50 values of 5.4 nM for AAK1 and 11.9 μM for hERG. HW161023 can suppress pain response in a rat model of chronic sciatic nerve compression injury.

MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.

7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. This compound inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. It disrupts PAR4-mediated aggregation and related signaling pathways, including NF-κB, Ca2+/protein kinase C (PKC), Akt, ERK, and p38. In a streptozotocin (STZ)-induced diabetic mouse model, 7,4'-Dimethoxy-3-hydroxyflavone inhibits vascular PAR4 expression, improves endothelial dysfunction, and reduces oxidative stress. Additionally, it prevents thrombosis in mice without affecting bleeding time.

PI4Kβ/PKG-IN-1 (Compound 19) is an orally active dual inhibitor targeting phosphatidylinositol 4-kinase β (PI4Kβ) and cGMP-dependent protein kinase (PKG) in Plasmodium. This compound exhibits potent antimalarial activity and holds promise for malaria research.

PI4Kβ/PKG-IN-2 (Compound 20) is an orally active dual inhibitor that targets phosphatidylinositol 4-kinase β (PI4Kβ) and cGMP-dependent protein kinase (PKG) in Plasmodium. It demonstrates significant inhibitory effects on Plasmodium and holds potential for use in malaria research.

p38 MAPK-IN-8 (Compound 8) is an orally active, potent, and selective inhibitor of p38 mitogen-activated protein kinase (p38 MAPK). It holds potential for research in inflammatory responses, autoimmune diseases, and cancer.