CDK Inhibitor

CDK8-IN-4 (Standard) is the analytical standard of CDK8-IN-4 (HY-111465). This product is intended for research and analytical applications. CDK8-IN-4 is an inhibitor of CDK8 extracted from patent WO2014090692A1, compound example 16, with an IC₅₀ of 0.2 nM.

MeBIO (Standard) is the analytical standard of MeBIO (HY-103221). This product is intended for research and analytical applications. MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC₅₀ of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively.

PROTAC CDK9 Degrader-1 (Standard) is the analytical standard of PROTAC CDK9 Degrader-1 (HY-103628). This product is intended for research and analytical applications. PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.

CCT68127 is an orally active CDK inhibitor. CCT68127 can be used in anti-cancer research.

Amantadine (hydrochloride) (Standard) is the analytical standard of Amantadine (hydrochloride). This product is intended for research and analytical applications. Amantadine (1-Adamantanamine) hydrochloride is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine hydrochloride inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine hydrochloride also has anti-orthopoxvirus and anticancer activity. Amantadine hydrochloride can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research.

Dinaciclib (Standard) is the analytical standard of Dinaciclib (HY-10492). This product is intended for research and analytical applications. Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC₅₀s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.

AZD4573 (Standard) is the analytical standard of AZD4573 (HY-112088). This product is intended for research and analytical applications. AZD4573 is a potent and highly selective CDK9 inhibitor (IC₅₀ of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies.

Momilactone B is an inhibitor of α-amylase and α-glucosidase, with an IC₅₀ of 146.85 μg/mL against Aspergillus oryzae α-amylase and an IC₅₀ of 612.03 μg/mL against Saccharomyces cerevisiae α-glucosidase. Momilactone B upregulates the expression of p21^Waf1/Cip1, reduces the kinase activity of Cdk4 and Cdk6, induces cell cycle arrest and apoptosis in cancer cells, and triggers irreversible cell death via cell membrane damage. Momilactone B inhibits the growth of neighboring plant species and serves as a major contributing factor to the allelopathy of rice. Momilactone B can be used in studies related to rice allelopathy, type 2 diabetes, colon cancer and leukemia.

Antitrypanosomal agent 31 is an antitrypanosoma agent with a pEC50 of 6.4. Antitrypanosomal agent 31 inhibits GSK-3β, CDK-2, and CDK-4 with pIC₅₀s of 5.8, 6.9, and 7.1, respectively. Antitrypanosomal agent 31 can be used for the research of human african trypanosomiasis.

CGP60474 (Standard) is the analytical standard of CGP60474 (HY-11009). This product is intended for research and analytical applications. CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent K_inase (CDK) inhibitor (IC₅₀ values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.

(-)-Enitociclib (Standard) is the analytical standard of (-)-Enitociclib (HY-103019B). This product is intended for research and analytical applications. (-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.

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.

CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC₅₀ of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1^SER727 with an IC₅₀ of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC₅₀ of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57%.

P18IN011 is an inhibitor that specifically targets the interaction between p18(INK4C) and CDK6, with an IC₅₀ of 3.61 μM against mouse p18INK4C. P18IN011 relieves p18-mediated CDK6 inhibition, thereby effectively regulating the G1 phase cell cycle checkpoint. P18IN011 significantly enhances the proliferation, self-renewal and bone marrow reconstitution abilities of hematopoietic stem cells, and increases the frequency of primitive hematopoietic cells to promote cobblestone area formation. Acting specifically on p18-expressing hematopoietic cells via CDK4/6, P18IN011 not only supports the ex vivo expansion of human umbilical cord blood hematopoietic stem cells, but also maintains their long-term reconstitution capacity during in vitro culture to enable multi-lineage transplantation.

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.

RKS262 is an orally active cyclin/CDK inhibitor. RKS262 is also an apoptosis inducer and cell cycle regulator, exhibiting cytotoxic activity against cancer cells. RKS262 induces caspase-3 cleavage, ROS generation, SAPK/JNK activation, and upregulates the expression of p53, Bid, Bad, Bok, and p27. RKS262 inhibits the expression of Bcl-2, Mcl-1, Bcl-xL, p21, cyclin D1, cyclin B1, cdc-2, cyclin D4, and DNA-pk KU-80 subunit. RKS262 suppresses the phosphorylation of the IGF-1R/PI3K/PKC pathway, ras oncogene activity, and Cdk-6, while increasing total Akt expression. RKS262 induces G₂/M or S phase cell cycle arrest, disrupts mitochondrial transmembrane potential, and reduces tumor burden in xenograft models. RKS262 is used in research on neuroblastoma and ovarian cancer.