CDK Inhibitor

Cdc7-IN-1 (Standard) is the analytical standard of Cdc7-IN-1 (HY-101523). This product is intended for research and analytical applications. Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death.

R547 (Standard) is the analytical standard of R547 (HY-10014). This product is intended for research and analytical applications. R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

PHA-793887 (Standard) is the analytical standard of PHA-793887 (HY-11001). This product is intended for research and analytical applications. PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC₅₀s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase K_inase 3β with an IC₅₀ of 79 nM.

CDK8/19-IN-1 (Standard) is the analytical standard of CDK8/19-IN-1 (HY-111427). This product is intended for research and analytical applications. CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC₅₀s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.

AZD-5438 (Standard) is the analytical standard of AZD-5438. This product is intended for research and analytical applications. AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .

DS96432529 (Standard) is the analytical standard of DS96432529 (HY-145121). This product is intended for research and analytical applications. DS96432529 is an orally active CDK8 inhibitor with an IC₅₀ of 33 nM. DS96432529 enhances ALPase activity, with an EC₂₀₀ of 63 nM. DS96432529 inhibits TNF-α-induced activation of the RLR signaling pathway, activates mitophagy, accelerates mineralized nodule formation, and suppresses the proliferation of periodontal ligament stem cells. DS96432529 promotes bone formation, alleviates ligation-induced alveolar bone loss, and increases bone mineral density in ovariectomized animal models. DS96432529 can be used in studies related to periodontitis and osteoporosis.

THZ1 (Standard) is the analytical standard of THZ1 (HY-80013). This product is intended for research and analytical applications. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM. THZ1 also inhibits the closely related K_inases CDK12 and CDK13 and downregulates MYC expression.

(R)-Roscovitine (Standard) is the analytical standard of (R)-Roscovitine (HY-30237). This product is intended for research and analytical applications. (R)-Roscovitine (Seliciclib) is an orally bioavailable, selective and BBB-permeable CDKs inhibitor with IC₅₀s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.

Romaciclib monohydrochloride (Standard) is the analytical standard of Romaciclib (monohydrochloride) (HY-111388A). This product is intended for research and analytical applications. SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits K_inase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.

CLK1-IN-1 (Standard) is the analytical standard of CLK1-IN-1 (HY-103082). This product is intended for research and analytical applications. CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 (CLK1) inhibitor, with an IC₅₀ of 2 nM.

Fucoxanthinol, a carotenoid, is a deacetylated Fucoxanthin (HY-N2302) metabolite with oral activity, and inhibits rat pancreatic lipase with an IC₅₀ of 764 nM. Fucoxanthinol reduces expression of Bcl-2, Bcl-xL, survivin, XIAP, cIAP2, cyclin D1, cyclin D2, cyclin E, CDK4, CDK6, β-catenin, JunD, PPARγ, and induces GADD45α expression. Fucoxanthinol activates caspase-3, caspase-8, caspase-9, Nrf2/Keap1/ARE pathway, and inhibits activation of Akt, NF-κB, AP-1, PDPK1, GSK3β phosphorylation. Fucoxanthinol induces apoptosis, G0/G1 cell cycle arrest, inhibits cancer cell viability, proliferation, migration, invasiveness, tumour growth, adipocyte differentiation, oxidative stress, neurotoxicity, triglyceride absorption, angiogenesis, and obesity-induced inflammation. Fucoxanthinol can be used for the research of osteosarcoma, leukemia, lymphoma, adult T-cell leukemia, prostate cancer, colon cancer, breast cancer, hypertriglyceridaemia, Alzheimer’s disease, Parkinson’s disease, obesity, insulin resistance, malignant melanoma, and type II diabetes.

CA224 (Standard) is the analytical standard of CA224 (HY-111207). This product is intended for research and analytical applications. CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC₅₀ of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.

CDK9-IN-1 (Standard) is the analytical standard of CDK9-IN-1. This product is intended for research and analytical applications. CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.

Purvalanol A (Standard) is the analytical standard of Purvalanol A. This product is intended for research and analytical applications. Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.

PF 477736 (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

(R)-DRF053 is a CDK inhibitor. (R)-DRF053 inhibits Cdk5 and promotes the formation of ductal precursor β cells. (R)-DRF053 inhibits Dil-ox-LDL uptake and CD36 gene expression induced by advanced glycation end products (AGEs) in U937 cells.

NG 52 (Standard) is the analytical standard of NG 52. This product is intended for research and analytical applications. NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p.

NSC 625987 (Standard) is the analytical standard of NSC 625987 (HY-103380). This product is intended for research and analytical applications. NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC₅₀ of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.

Flavopiridol (Standard) is the analytical standard of Flavopiridol (HY-10005). This product is intended for research and analytical applications. Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.

Fadraciclib (Standard) is the analytical standard of Fadraciclib (HY-101212). This product is intended for research and analytical applications. Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively.