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CDK9 kinase activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	CDK (23) Apoptosis (8) Bcl-2 Family (2) Biochemical Assay Reagents (1) c-Myc (1) Casein Kinase (1) Caspase (1) COX (1) DNA/RNA Synthesis (1) EGFR (1) FLT3 (1) GSK-3 (2) IAP (1) JAK (3) Ligands for Target Protein for PROTAC (1) MEK (2) PARP (1) PROTACs (1) Target Protein Ligand-Linker Conjugates (1)
By Research Areas:	Cancer (23) Infection (1) Inflammation/Immunology (1) Neurological Disease (1)

Targets Recommended: CDK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12214A

NVP-2 Maximum Cited Publications 41 Publications Verification	CDK Apoptosis	Cancer
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC₅₀ of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC₅₀ values of 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces cell apoptosis.

HY-137478

KB-0742 3 Publications Verification	CDK	Cancer
KB-0742 is a potent, selective and orally active *CDK9* inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity .

HY-15504A

RGB-286638 free base 3 Publications Verification	CDK GSK-3 MEK JAK	Cancer
RGB-286638 is a *CDK* inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and *p35-CDK5* with IC₅₀s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC₅₀s of 3, 5, 50, and 54 nM.

HY-111388A

Romaciclib monohydrochloride 5+ Cited Publications SEL120-34A monohydrochloride	CDK	Cancer
SEL120-34A monohydrochloride is an ATP-competitive and selective *CDK8* inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726 . Has anti-tumor activity .

HY-15504

RGB-286638 3 Publications Verification	CDK GSK-3 MEK JAK	Cancer
RGB-286638 is a *CDK* inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and *p35-CDK5* with IC₅₀s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC₅₀s of 3, 5, 50, and 54 nM.

HY-137478A

KB-0742 dihydrochloride 3 Publications Verification	CDK	Cancer
KB-0742 dihydrochloride is a potent, selective and orally active *CDK9* inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 dihydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity .

HY-16559

Riviciclib hydrochloride 3 Publications Verification P276-00	CDK Apoptosis	Cancer
Riviciclib hydrochloride (P276-00) 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 hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells .

HY-123955

Casein Kinase inhibitor A86	Casein Kinase CDK Apoptosis	Cancer
Casein Kinase inhibitor A86 is a potent and orally active *casein kinase* 1α (CK1α)** inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities .

HY-151071

TMX-3013	Ligands for Target Protein for PROTAC CDK	Cancer
TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC₅₀ values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs) .

HY-119715

AG-012986	CDK Apoptosis	Inflammation/Immunology Cancer
AG-012986 is a pan-CDK inhibitor with K_i values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces K_i-67 expression. AG-012986 exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity .

HY-178861

dCDK9-202	PROTACs CDK Caspase PARP Apoptosis	Cancer
dCDK9-202 a potent CDK9 PROTAC degrader with an DC₅₀ value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)) .

HY-201330

GDC-4198 RGT-419B	CDK	Cancer
GDC-4198 (RGT-419B) is an orally active *CDK4/2* inhibitor with desired degrees of selectivity against kinases such as CDK6, CDK9 and GSK3β. GDC-4198 inhibits the activity of cyclin-CDK complexes, blocks phosphorylation of the retinoblastoma protein (pRb), arresting the cell cycle transition from G1 to S phase. GDC-4198 is promising for research of cancers, such as breast cancer (especially hormone receptor-positive, HER2-negative type), lung cancer, and colorectal cancer .

HY-16559A

Riviciclib P276-00 free base	CDK	Cancer
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-178499

CDK9-IN-44	CDK c-Myc Bcl-2 Family	Neurological Disease Cancer
CDK9-IN-44 (Compound 7) is a selective *CDK9* inhibitor (IC₅₀=7.6 μM). CDK9-IN-44 inhibits CDK9/cyclin T1 kinase activity, blocking transcriptional elongation, reducing the expression of pro-cancer proteins (such as MCL1, c-MYC), and inducing tumor cell apoptosis. CDK9-IN-44 is promising for research of glioblastoma (GBM) and central nervous system (CNS) disorders .

HY-137478B

KB-0742 hydrochloride	CDK	Cancer
KB-0742 hydrochloride is a potent, selective and orally active *CDK9* inhibitor with an IC₅₀ of 6 nM for CDK9/cyclin T1. KB-0742 hydrochloride is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 hydrochloride has potent anti-tumor activity .

HY-147905

CDK9-IN-18	CDK Apoptosis	Cancer
CDK9-IN-18 is a potent *CDK9* inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.

HY-136841

SLM6	CDK	Cancer
SLM6 is a sangivamycin-like molecule. SLM6 is a *CDK9* inhibitor. SLM6 inhibits CDK9/cyclin K and CDK9/cyclin T1 kinase activity with IC₅₀s of 280 nM and 133 nM, respectively. SLM6 also inhibits CDK1/cyclin B and CDK2/ cyclin A with IC₅₀s of less than 300 nM. SLM6 induces apoptosis in multiple myeloma (MM) cells .

HY-147794

CDK9-IN-41	CDK COX EGFR	Cancer
CDK9-IN-41 is a potent *CDK9, EGFR, HER2, and COX-2* kinases inhibitor with IC₅₀s of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM. COX-2-IN-18 exhibits remarkable antitumor activity against leukemia cancer cells, colon cancer cells, melanoma cells, ovarian cells and breast cells .

HY-151375

CDK9/10/GSK3β-IN-1	CDK	Cancer
CDK9/10/GSK3β-IN-1 (compound 13c) is a *kinase* inhibitor (Flavopiridol (HY-10005) analogue) that effectively inhibits HsGSK3β (IC₅₀=59 nM), HsCDK9/CyclinT (IC₅₀=64 nM), HsCDK5/p25 (IC₅₀=1.093 μM) and HsCDK2/CyclinA (IC₅₀=1.725 μM). CDK9/10/GSK3β-IN-1 has anti-cancer cellular activity comparable to or higher than that of Flavopiridol. CDK9/10/GSK3β-IN-1 shows high anti-proliferative activity in vitro against up to seven cancer cell lines .

HY-161768

VCC972839:01	CDK Apoptosis	Cancer
VCC972839:01 is an inhibitor for cyclin dependent kinase (CDK9), with IC₅₀ of 7 nM. VCC972839:01 inhibits the cell viability of SCLC cells in nanomolar levels. VCC972839:01 induces apoptosis through an intrinsic pathway. VCC972839:01 exhibits antitumor activity in mouse model .

HY-15163A

Zotiraciclib hydrochloride	FLT3 JAK CDK	Cancer
Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies .

HY-178862

CDK9 ligand-Linker Conjugate	Target Protein Ligand-Linker Conjugates	Cancer
CDK9 ligand-Linker Conjugate is a synthesized CDK9 ligand-linker conjugate that can be used for synthesis of dCDK9-202 (HY-178861). dCDK9-202 is a potent CDK9 PROTAC degrader with anti-tumor activity .

HY-179633

ZLMT-72	CDK Apoptosis DNA/RNA Synthesis Bcl-2 Family IAP	Cancer
ZLMT-72 is an orally active dual *CDK2* and *CDK9* inhibitor with IC₅₀s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI₅₀ < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC) .

HY-182470

AG-012986 dihydrochloride	CDK
AG-012986 (dihydrochloride) is a pan-CDK inhibitor with K_i values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC₅₀ values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces K_i-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity .

HY-126773

Dp2mT	Biochemical Assay Reagents	Infection
Dp2mT is a non-cytotoxic control compound, with an IC₅₀ of >3 μM for HIV-1 transcription inhibition and an IC₅₀ of >10 μM for cytotoxicity. Dp2mT does not bind to intracellular iron pools. Dp2mT does not inhibit CDK9 activity .

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CDK9 kinase activity

Inhibitors & Agonists