CDK Inhibitor

CDK2-IN-61 is a highly selective CDK2 inhibitor with a human IC₅₀ of 0.25 nM. CDK2-IN-61 can be used in cancer-related research.

Fadraciclib (Standard) is the analytical standard of Fadraciclib (HY-101212). This product is intended for research and analytical applications. Fadraciclib (CYC065) is a second-generation, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50s of 5 and 26 nM, respectively.

6-(Dimethylamino) purine (6-Dimethylaminopurine) is a serine threonine protein kinase inhibitor. 6-(Dimethylamino) purine can inhibit prolactin induced expression of lactoprotein genes in rabbit mammary gland cells. 6-(Dimethylamino) purine can affect the maturation of mammalian oocytes. 6-(Dimethylamino) purine can lead to downregulation of genes related to cell proliferation and cell cycle progression, such as proliferating cell nuclear antigen, insulin-like gene 1, and serine protease inhibitor 2 genes, and induce apoptosis in lymphoma cells (apoptosis).

Clausine Z (1,6-Dihydroxy-9H-carbazole-3-carboxaldehyde) is an alkaloid CDK5 inhibitor isolated from the plant from Momordica charantia.

Tagtociclib hydrate (Standard) is the analytical standard of Tagtociclib hydrate (HY-137894A). This product is intended for research and analytical applications. PF-07104091 hydrate is a potent and selective CDK2/cyclin E₁ and GSK3β inhibitor, with K_is of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E₁-amplified cancers. (patent WO2020157652A2).

FIT-039 (Standard) is the analytical standard of FIT-039. This product is intended for research and analytical applications. FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.

NS-0011 is a CDK5 inhibitor with a K_d value of 16 μM. NS-0011 binds to the nuclear export signal domain of CDK5, disrupts its interaction with CRM-1 and increases the accumulation of CDK5 in the nucleus. NS-0011 inhibits the proliferation of gastric cancer cells. NS-0011 suppresses the occurrence of gastric cancer xenograft tumors. NS-0011 is applicable to gastric cancer-related research.

Enitociclib (Standard) is the analytical standard of Enitociclib (HY-103019). This product is intended for research and analytical applications. Enitociclib ((+)-BAY-1251152; (+)-VIP152) is a selective CDK9 inhibitor (IC₅₀=3 nM) that inhibits transcriptional elongation by blocking Ser2/Ser5 phosphorylation of RNA polymerase II. Enitociclib specifically depletes key short-lived proteins such as c-MYC, MCL-1 and induces tumor cell apoptosis. Enitociclib also interferes with the production of enhancer RNAs (eRNA) and enhancer-promoter interactions, and downregulates oncogene expression at the epigenetic level. Enitociclib exerts synergistic effects with agents including Bortezomib (HY-10227), Lenalidomide (HY-A0003), Pomalidomide (HY-10984), Venetoclax (HY-15531) and Paclitaxel (HY-B0015), and even reverses paclitaxel resistance. Enitociclib serves as a vital research tool for various malignancies such as double-hit diffuse large B-cell lymphoma, multiple myeloma and pancreatic ductal adenocarcinoma.

SNS-032 (Standard) is the analytical standard of SNS-032. This product is intended for research and analytical applications. SNS-032 (BMS-387032) is a potent and selective inhibitor of?CDK2, CDK7, and CDK9 with?IC50s?of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect.

Nimbolide (Standard) is the analytical standard of Nimbolide. This product is intended for research and analytical applications. Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.

CDK4-IN-8 is a selective CDK4 inhibitor with no activity against CDK6, and it inhibits the proliferation of breast cancer cells. CDK4-IN-8 can be used in breast cancer-related research.

(±)-Enitociclib (Standard) is the analytical standard of (±)-Enitociclib (HY-103019A). This product is intended for research and analytical applications. (±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). 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.

JH-XI-10-02 (Standard) is the analytical standard of JH-XI-10-02 (HY-111518). This product is intended for research and analytical applications. JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC₅₀ of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.

Ro-3306 (Standard) is the analytical standard of Ro-3306 (HY-12529). This product is intended for research and analytical applications. Ro-3306 is a potent and selective inhibitor of CDK1, with K_is of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.

MG-002 is an orally active eIF4A1 and eIF4A2 inhibitor with a human eIF4A1 IC₅₀ of 43 nM. MG-002 prevents competent ribosome recruitment to mRNA, inhibits cap-dependent mRNA translation, and engages eIF4A2 via the same RNA clamping mechanism to inhibit mRNA translation. MG-002 induces G2/M cell cycle delay, induces apoptosis, suppresses synthesis of c-MYC and cyclin D1, and shows minimal overt toxicity in mice. MG-002 inhibits primary triple-negative breast cancer tumor growth, attenuates metastatic spread, and enhances anti-neoplastic activity of Doxorubicin (HY-15142A) in pre-clinical models.

Simurosertib (Standard) is the analytical standard of Simurosertib (HY-100888). This product is intended for research and analytical applications. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.

Aminopurvalanol A (Standard) is the analytical standard of Aminopurvalanol A (HY-104013). This product is intended for research and analytical applications. Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization.

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.