CDK Inhibitor

Samuraciclib hydrochloride (Standard) is the analytical standard of Samuraciclib hydrochloride (HY-103712A). This product is intended for research and analytical applications. Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects.

THZ531 (Standard) is the analytical standard of THZ531 (HY-103618). This product is intended for research and analytical applications. THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC₅₀s of 158 nM and 69 nM, respectively.

CC-671 (Standard) is the analytical standard of CC-671 (HY-108709). This product is intended for research and analytical applications. CC-671 is a dual TTK protein K_inase/CDC2-like K_inase (CLK2) inhibitor with IC₅₀s of 0.005 and 0.006 μM for TTK and CLK2, respectively.

3MB-PP1 (Standard) is the analytical standard of 3MB-PP1 (HY-102069). This product is intended for research and analytical applications. 3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC₅₀=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division.

AT7519 (Standard) is the analytical standard of AT7519. This product is intended for research and analytical applications. AT7519 (AT7519M) as a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.

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.

CDK12-Cyclin K ligand-1 is a ligand of PROTAC degrader that binds to the E3 ligase. CDK12-Cyclin K ligand-1 can be used in the synthesis of PROTAC degrader such as PP-C8 (HY-144691).

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.

Alisol B 23-acetate (Standard) is the analytical standard of Alisol B 23-acetate (HY-N0805). This product is intended for research and analytical applications. Alisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma.

JTK-101 is a selective HIV inhibitor. JTK-101 selectively reduces HIV-1 mRNA synthesis by inhibiting Tat cofactors, including CDK9 and cyclin T1, thereby suppressing the transcriptional activity of HIV-1. JTK-101 may be used in the field of anti-HIV virus research.

WEE1-IN-15 is an ATP-competitive, selective WEE1 kinase inhibitor (IC₅₀: 42 nM). WEE1-IN-15 abolishes CDK1 phosphorylation. WEE1-IN-15 induces DNA damage and replication stress, and increases the S-phase cell population. WEE1-IN-15 shows selective anticancer effects on colorectal cancer organoids. WEE1-IN-15 can be used for research on colorectal cancer.

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.