CDK Inhibitor

CDK Inhibitors (1014):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-112243

Cimpuciclib	Inhibitor
Cimpuciclib is a selective CDK4 inhibitor (IC₅₀: 0.49 nM) that has anti-tumor activity.

HY-130516

Cdc7-IN-4	Inhibitor
Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

HY-151407

CDK1-IN-3	Inhibitor
CDK1-IN-3 (8g) is a selective CDK1 inhibitor with IC₅₀s of 36.8, 305.17 and 369.37 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-3 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-3 can be used for the research of cancer.

HY-143497

HDAC1/2 and CDK2-IN-1	Inhibitor
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC₅₀ values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.

HY-182906

XL495	Inhibitor
XL495 is an potent, selective and orally active PKMYT1 inhibitor. XL495 inhibits CDK1 Thr14 phosphorylation and induces KAP1 Ser824 phosphorylation in xenograft tumors. XL495 reduces tumor growth in colorectal and breast cancer xenograft models, and achieves tumor regression with DNA-damaging agents in colorectal cancer xenograft models. XL495 can be used for the research of cancer, such as breast cancer and colorectal cancer.

HY-19718

OTS964	Inhibitor
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC₅₀ of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a K_d of 40 nM.

HY-151436

ZLMT-12	Inhibitor
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC₅₀ values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC₅₀=19.023 μM) and BChE (IC₅₀=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.

HY-136711

CDK7-IN-2 hydrochloride hydrate	Inhibitor
CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and selective CDK7 inhibitor. CDK7-IN-2 has potent anti-cancer activity.

HY-110368

BS-181 dihydrochloride	Inhibitor
BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC₅₀=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC₅₀ values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC₅₀=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy.

HY-111537

rel-AZ5576	Inhibitor
rel-AZ5576 is a selective CDK9 inhibitor with the activity of downregulating Mcl-1 and MYC mRNA transcription and protein expression in diffuse large B-cell lymphoma by inhibiting CDK9, promoting MYC protein turnover, reducing MYC phosphorylation on the stable Ser62 residue and downregulating MYC transcriptional targets, inhibiting the growth of diffuse large B-cell lymphoma cell lines in vitro and in vivo and independent of the cell origin.

HY-126244

CDK4/6-IN-3	Inhibitor
CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with K_is of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a K_i of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.

HY-171334A

P1D-34	Inhibitor
P1D-34 is a Pin1 PROTAC degrader with a DC₅₀ value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883).

HY-130001

CDK9-IN-9	Inhibitor
CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC₅₀ of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC₅₀ of 155 nM. CDK9-IN-9 has anti-cancer activity.

HY-145655

CDK7-IN-11	Inhibitor
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC₅₀ value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7.

HY-149641

CDK9-IN-29	Inhibitor
CDK9-IN-29 (compound Z11) is a potent CDK9 inhibitor (IC₅₀ = 3.20 nM) with good kinase selectivity. CDK9-IN-29 inhibits cell proliferation and induces apoptosis.

HY-16559A

Riviciclib	Inhibitor
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC₅₀s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib shows antitumor activity on cisplatin-resistant cells.

HY-130515

Cdc7-IN-3	Inhibitor
Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.

HY-131063

CDK6/9-IN-1	Inhibitor
CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC₅₀ values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.

HY-156646

Tibremciclib	Inhibitor
Tibremciclib is a CDK4 inhibitor with antineoplastic activity.

HY-15681A

Senexin A hydrochloride	Inhibitor
Senexin A hydrochloride is an inhibitor of CDK8/19 (IC₅₀: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.

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