CDK Inhibitor

5-Iodo-indirubin-3'-monoxime (Standard) is the analytical standard of 5-Iodo-indirubin-3'-monoxime (HY-111930). This product is intended for research and analytical applications. 5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the K_inase, with IC₅₀s of 9, 20 and 25 nM, respectively.

OM137 is an aurora kinase inhibitor, with an IC₅₀ of 21.7 μM (Aurora A kinase) and 2.4 μM (Aurora B kinase). OM137 also inhibits Cdk1/cyclinB and Cdk5/p25 with an approximate IC₅₀ of 20 μM. OM137 reduces spindle checkpoint-signaling proteins (Mad2 and BubR1) at the kinetochores of chromosomes.

CDK9-IN-8 (Standard) is the analytical standard of CDK9-IN-8 (HY-102039). This product is intended for research and analytical applications. CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC₅₀ of 12 nM.

Epmedin C (Standard) is the analytical standard of Epmedin C. This product is intended for research and analytical applications. Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia.

FN-1501 (Standard) is the analytical standard of FN-1501 (HY-111361). This product is intended for research and analytical applications. FN-1501 is a potent inhibitor of FLT3 and CDK, with IC₅₀s of 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively. FN-1501 has anticancer activity.

Daphnoretin (Dephnoretin; Thymelol) (Standard) is the analytical standard of Daphnoretin (HY-N0699). This product is used for research and analytical applications. Daphnoretin is a protein kinase C (PKC) activator that can inhibit the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and has antiviral activity. Daphnoretin exerts its anti-tumor effect by inhibiting the activation of the PI3K/AKT signaling pathway, triggering the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and the activation of the NLRP3 inflammasome. Daphnoretin can regulate the differentiation and maturation of dendritic cells, by down-regulating the phosphorylation level of JNK, inhibiting its immune stimulating function, thereby playing a protective role in skin transplant rejection reactions.

NU6140 (Standard) is the analytical standard of NU6140 (HY-107419). This product is intended for research and analytical applications. NU6140 is a selective CDK2-cyclin A inhibitor (IC₅₀, 0.41 μM), exhibits 10- to 36-fold selectivity over other CDKs. NU6140 also potently inhibits Aurora A and Aurora B, with IC₅₀s of 67 and 35 nM, respectively. Enhances the apoptotic effect, with anti-cancer activity.

BML-259 (Standard) is the analytical standard of BML-259 (HY-108348). This product is intended for research and analytical applications. BML-259 is a potent cyclin-dependent K_inase 5 (Cdk5) inhibitor, with IC₅₀s of 64 and 98 nM for Cdk5 and Cdk2, respectively.

Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.

K00546 (Standard) is the analytical standard of K00546 (HY-103647). This product is intended for research and analytical applications. K00546 is a potent CDK1 and CDK2 inhibitor with IC₅₀s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. K00546 is also a potent CDC2-like kinase 1 (CLK1) and CLK3 inhibitor with IC₅₀s of 8.9 nM and 29.2 nM, respectively.

Palbociclib-d₄ is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC₅₀ values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma.

Protein kinase inhibitor 13 (Compound I-90) is the inhibitor for protein kinase that exhibits inhibitory effects on kinases such as PIM-1, CDK-2, GSK-3 and SRC.

Senexin B (Standard) (SNX2-1-165 (Standard)) is the analytical standard of Senexin B (HY-101800). This product is intended for research and analytical applications. Senexin B (SNX2-1-165; BCD-115) is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with Kds of 140 nM for CDK8 and 80 nM for CDK19.

Trilaciclib (hydrochloride) (Standard) is the analytical standard of Trilaciclib (hydrochloride). This product is intended for research and analytical applications. Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC₅₀s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

WAY-643018 (Compound 2), an indazolecarboxamide derivative, is a CDK1, CDK2, and CDK4 inhibitor. CDK1/2/4-IN-2 has the potential for cancer research.

PKMYT1-IN-7 (compound 7) is an orally active PKMYT1 inhibitor with IC₅₀ values of 1.6 nM and 0.06 μM against of PKMYT1 and pCDK1, respectively. PKMYT1-IN-7 suppresses the phosphorylation of CDK1 at T14 and Y15. PKMYT1-IN-7 shows anticancer activity both < and <.