CDK Inhibitor

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.

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.