CDK Inhibitor

Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.

CDK9-IN-30 is a CDK9 inhibitor that inhibits HIV-1 viral replication.

ABC1183 (Standard) is the analytical standard of ABC1183 (HY-100950). This product is intended for research and analytical applications. ABC1183 is an orally active selective dual GSK3 and CDK9 inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC50 values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities.

CDK2-IN-39 (compound 4) is a CDK2 inhibitor.

GDC-0425 hydrochloride (RG-7602 hydrochloride) is an orally active, highly selective ChK1 inhibitor. GDC-0425 hydrochloride abrogates cell cycle arrest and inhibits genomic repair. GDC-0425 hydrochloride potently suppresses Gemcitabine (HY-17026)-induced pCDK1/2 expression. GDC-0425 hydrochloride can be used in research related to osteosarcoma, ovarian cancer, basal (triple-negative) breast cancer, and colorectal cancer.

CDK8-IN-1 (Standard) is the analytical standard of CDK8-IN-1 (HY-103492). This product is intended for research and analytical applications. CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC₅₀ of 3 nM.

Abemaciclib metabolite M2 (Standard) is the analytical standard of Abemaciclib metabolite M2. This product is intended for research and analytical applications. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s of 1.2 and 1.3 nM, respectively. Anti-cancer activity[1][2].

CDK2-IN-21 (example 30) is a potent cyclin-dependent kinase 2 (CDK2) inhibitor with an IC₅₀ of 0.24 µM. CDK2-IN-21 can be used for cancer research.

Milciclib (Standard) is the analytical standard of Milciclib. This product is intended for research and analytical applications. Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

GSK 3 Inhibitor IX (Standard) is the analytical standard of GSK 3 Inhibitor IX (HY-10580). This product is intended for research and analytical applications. GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC₅₀s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

Alaternin (Catharticin) is an anthraquinone compound with antioxidant and hepatoprotective activities. Alaternin has an inhibitory activity against hydroxyl radicals generated in a cell-free chemical system (FeSO₄/H₂O₂) with an IC₅₀ value of 3.05 μM. Alaternin exhibits hepatoprotective activity against Tacrine (HY-111338)-induced toxicity in human hepatic HepG2 cells with an EC₅₀ value of 4.02 μM.

CK7 (Standard) is the analytical standard of CK7 (HY-103646). This product is intended for research and analytical applications. CK7, a Cdk2/9 inhibitor, can be used for the synthesis of Nek1 inhibitor BSc5231 and BSc5367.

R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with K_is of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

Ibulocydine is an isobutyrate prodrug of the Cdk inhibitor BMK-Y101 (HY-188159), with oral activity, and exhibits IC₅₀ values of approximately 50 nM against CDK1/CDK2, 530 nM against CDK7/cyclin H/Mat1, and 85 nM against CDK9/cyclin T. Ibulocydine reduces the phosphorylation levels of Rb, nucleolin, and RNA polymerase II CTD Ser-5 and Ser-2, downregulates the expression of Mcl-1, survivin, and XIAP, decreases MMP-9 expression, and lowers the Bcl-2/Bax ratio, activates calpain-mediated Bax cleavage, cytochrome c release, and caspase activation. Ibulocydine induces apoptosis, inhibits the growth of cancer cells and xenografts, enhances the sensitivity of cancer cells to TRAIL and radiotherapy, and blocks cancer cell metastasis. Ibulocydine can be used in research related to various cancers, including hepatocellular carcinoma, triple-negative breast cancer, lung cancer, and colon cancer.

ZK 304709 is a multi-target CDK inhibitor.

CDKi free base is a CDK inhibitor. CDKi free base induces morphological changes, DNA fragmentation, and cell death in vestibular schwannoma cells. CDKi free base downregulates pRb, EGF-R, PI3K, NF-κB, and Shh levels, while upregulating JNK, ASK1, Caspase 3, and p21, and induces PARP-1 cleavage. CDKi free base can be used in research related to vestibular schwannoma.

Trilaciclib (Standard) is the analytical standard of Trilaciclib (HY-101467). This product is intended for research and analytical applications. Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy.

Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields.