CDK Inhibitor

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.