kinase-3

PF-04802367 is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. It shows desirable central nervous system (CNS) properties and potency. It is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively.

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2, demonstrating an IC50 of 1 nM.

Multi-kinase inhibitor 3 (compound 12) is an orally active and effective multikinase (multikinase) inhibitor, demonstrating potent IC50 values against FLT1 VEGFR1, KDR VEGFR2, FLT4 VEGFR3, FLT3, PDGFRα, and PDGFRβ, at 1.59, 1.23, 1.19, 0.59, 0.22, and 1.15 nM respectively. This compound exhibits anti-proliferative and anticancer activities.

Multi-target kinase inhibitor 3 (compound 6i) is a potent multi-target anticancer agent.

ATRkinase-IN-3 (Compound I-G-28) is an inhibitor of the ATR protein kinase, exhibiting a Ki value ranging from 0.01 to 1 μM, and is utilized in cancer research.

Protein kinase G inhibitor-3 (Compound 177) is an inhibitor of mycobacterial serine threonine protein kinases. It is utilized in the research of diseases associated with mycobacterial infections.

PDGFRαkinase inhibitor 3 (Compound L7) is a potent inhibitor targeting the PDGFRαD842V kinase, exhibiting IC50 values of 23.8 nM in biochemical assays and 2.1 nM in cellular assays. It binds to the ATP binding site of PDGFRαD842V, blocking downstream signaling pathways and inhibiting kinase activity. PDGFRαkinase inhibitor 3 is applicable in gastrointestinal stromal tumor (GIST) research.

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

Pim-1 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase with an inhibitory concentration (IC50) of 35.13 nM [1].

MET kinase-IN-3 is a potent, orally active MET inhibitor (IC50: 9.8 nM) that exhibits good broad-spectrum anti-proliferative effects on cancer cells.

IRE1α kinase-IN-3 is a potent, ATP-competitive inhibitor of IRE1α (Ki: 480 nM).

Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor, targeting VEGFR-2 with an IC50 of 58.3 nM and PDGFRβ with an IC50 of 55 nM.

Casein kinase 1δ-IN-3 (Compound 23a) is an inhibitor of casein kinase 1 delta (CK1δ) with a pIC50 of 6.5376 M.

TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, is a potent inhibitor of tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

BCR-ABL kinase-IN-3 (example 1), a potent BCR-ABL inhibitor, is significant in the study of acute myeloid leukemia (AML) [1].

EGFR kinase inhibitor 3 (compound 2) serves as a dual-action inhibitor targeting both ATP and allosteric sites of the EGFR kinase, exhibiting potent IC50 values of less than 10 nM for wild-type EGFR, 1.5 nM for the L858R mutation, 0.059 nM for the L858R T790M mutation, and 0.064 nM for the L858R T790M C797S mutation. It is classified as a C-linked inhibitor [1].

Casein Kinase Substrates 3 (CKS3) is a substrate of casein kinase (CK).

BCR-ABLkinase-IN-3 (dihydrochloride) (example 1) is an effective inhibitor of BCR-ABL, playing a significant role in research on acute myeloid leukemia (AML).

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Recilisib (ON 01210) is a radioprotectant that activates AKT and PI3K activities in cells.