3-kinase

Zandelisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K)(p110δ, IC50 of 3.5 nM), and with antineoplastic activity.

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.

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).

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

PI3-Kinase α Inhibitor 2 (hydrochloride) is a PI3-Kinase α inhibitor.

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).

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.

Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

5-Fluorouracil (5-FU) is a uracil analog and inhibitor of DNA synthesis, exhibiting antitumor activity by affecting pyrimidine synthesis through thymidylate synthase inhibition; it induces apoptosis and autophagy.