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CDK9-IN-9

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) c-Myc (1) Casein Kinase (1) CDK (19) ERK (1) Ligands for Target Protein for PROTAC (1) Molecular Glues (2) PKC (1) PROTACs (2)
By Research Areas:	Cancer (20) Neurological Disease (2)

Targets Recommended: AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-100429

CAN508 1 Publications Verification
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC₅₀ of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity .

HY-137478A

KB-0742 dihydrochloride	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-130001

*CDK9-IN-9*	CDK	Cancer
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-156296

CDK9-Cyclin T1 PPI-IN-1	CDK Apoptosis	Cancer
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC₅₀: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .

HY-137478

KB-0742	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-115729A

*(R)-PROTAC CDK9* ligand-1**	Ligands for Target Protein for PROTAC CDK	Cancer
(R)-PROTAC CDK9 ligand-1 (Compound 19.4) is a *CDK9*-targeting degrader that can be used to synthesize PROTAC with antitumor 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-100950

ABC1183
ABC1183 is an orally active selective dual GSK3 and *CDK9* inhibitor. ABC1183 inhibits GSK3β, GSK3α and CDK9/cyclin T1 with the IC₅₀ values of 657 nM, 327 nM and 321 nM, respectively. ABC1183 has anti-inflammatory and anti-tumor activities .

HY-156084

LL-K9-3	CDK PROTACs Apoptosis c-Myc	Cancer
LL-K9-3 is a potent small-molecule degrader of CDK9-cyclin T1. LL-K9-3 has anti-proliferative and pro-apoptotic activities and suppresses downstream signaling of CDK9 and AR. Moreover, LL-K9-3 inhibits AR and Myc-driven oncogenic transcriptional programs .

HY-130665

TL12-186 1 Publications Verification	PROTACs CDK	Cancer
TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC₅₀=73 nM) and CDK9/cyclin T1 (IC₅₀=55 nM) .

HY-139328

CDK12-IN-5	CDK	Cancer
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC₅₀=173 μM) and CDK9/Cyclin T1 (IC₅₀=127 μM) at high ATP (2 mM) (WO2021116178A1) .

HY-119940

MC180295 (rel)-MC180295	CDK	Cancer
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC₅₀ of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect .

HY-139327

CDK12-IN-4	CDK	Cancer
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC₅₀>20 μM) and CDK9/Cyclin T1 (IC₅₀>20 μM) at high ATP (2 mM) (WO2021116178A1) .

HY-139329

CDK12-IN-6	CDK	Cancer
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC₅₀>20 μM) and CDK9/Cyclin T1 (IC₅₀>20 μM) at high ATP (2 mM) (WO2021116178A1) .

HY-108907

SR-1277	Casein Kinase	Cancer
SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC₅₀s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC₅₀s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .

HY-12214A

NVP-2 Maximum Cited Publications 24 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-12843

Bohemine 1 Publications Verification	CDK ERK	Cancer
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC₅₀s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC₅₀ of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities .

HY-11009

CGP60474 5 Publications Verification	CDK PKC	Cancer
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (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 .

HY-126251

CDK9-IN-7	CDK Apoptosis	Cancer
CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC₅₀=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC .

HY-112371

(S)-CR8	CDK	Cancer
(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC₅₀s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC₅₀ 0.40 μM) .

HY-18340

(R)-CR8 CR8, (R)-Isomer	Molecular Glues CDK Apoptosis	Neurological Disease Cancer
(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC₅₀=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .

HY-18340A

(R)-CR8 trihydrochloride CR8, (R)-Isomer trihydrochloride	Molecular Glues CDK Apoptosis	Neurological Disease Cancer
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC₅₀=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .

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CDK9-IN-9

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