Search Result
Results for "
CDK9 selective inhibitor
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-124639
-
|
CDK
|
Cancer
|
CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer .
|
-
-
- HY-102039
-
|
CDK
|
Cancer
|
CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM.
|
-
-
- HY-139980
-
|
CDK
|
Cancer
|
CDK9-IN-13 (compound 38) is potent and selective CDK9 inhibitor, with an IC50 of <3 nM. CDK9-IN-13 exhibits short half-lives in rodents .
|
-
-
- HY-13231
-
|
CDK
HIV
|
Infection
|
CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC50 of 39 nM for CDK9/CycT1, extracted from reference, compound 87.
|
-
-
- HY-12871C
-
BAY-1143572 S-Enantiomer
|
CDK
|
Cancer
|
Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, which inhibits CDK9/CycT1 with an IC50 of 16 nM.
|
-
-
- HY-143585
-
|
CDK
|
Cancer
|
CDK9-IN-14 is a potent and selective CDK9 inhibitor with IC50 of 6.92 nM. CDK9-IN-14 has a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and has a good selectivity and a low toxicity and few side effects .
|
-
-
- HY-162919
-
|
CDK
|
Cancer
|
YK-2168 is a differentiated selective inhibitor of CDK9 .
|
-
-
- HY-130001
-
|
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-149641
-
|
CDK
|
Cancer
|
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-162619
-
|
Apoptosis
CDK
|
Cancer
|
CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity .
|
-
-
- HY-150562
-
|
CDK
|
Cancer
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
-
- HY-156296
-
|
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-155153
-
|
Apoptosis
CDK
|
Others
|
CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research .
|
-
-
- HY-137478A
-
|
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-137478
-
|
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-12871B
-
BAY-1143572
|
CDK
|
Cancer
|
Atuveciclib (BAY-1143572) is a potent and highly selective, oral PTEFb/CDK9 inhibitor. Atuveciclib (BAY-1143572) inhibits CDK9/CycT1 with an IC50 of 13 nM .
|
-
-
- HY-12871
-
BAY-1143572 Racemate
|
CDK
|
Cancer
|
Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective, oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
|
-
-
- HY-126251
-
|
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-12871A
-
(+)-BAY-1143572
|
CDK
|
Cancer
|
(+)-Atuveciclib is the isomer of Atuveciclib (Racemate) (HY-12871). Atuveciclib Racemate (BAY-1143572 Racemate) is the racemate mixture of Atuveciclib. Atuveciclib is a potent and highly selective,oral P-TEFb/CDK9 inhibitor which supresses CDK9/CycT1 with an IC50 of 13 nM.
|
-
-
- HY-100429
-
CAN508
1 Publications Verification
|
CDK
|
Cancer
|
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-X0150
-
|
CDK
|
Cancer
|
JSH-150 is a highly selective and potent CDK9 inhibitor with an IC50 of 1 nM.
|
-
-
- HY-100950
-
|
GSK-3
CDK
|
Inflammation/Immunology
Cancer
|
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-119940
-
(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-112088
-
|
CDK
|
Cancer
|
AZD4573 is a potent and highly selective CDK9 inhibitor (IC50 of <4 nM) that enables transient target engagement for the treatment of hematologic malignancies .
|
-
-
- HY-143584
-
|
CDK
|
Cancer
|
AZ5576 is a potent and highly selective CDK9 inhibitor (IC50: <5 nM). AZ5576 can be used for hematological Malignancy research .
|
-
-
- HY-103019B
-
(R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152
|
CDK
|
Cancer
|
(-)-Enitociclib ((R)-Enitociclib) is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
|
-
-
- HY-149673
-
|
CDK
|
Cancer
|
XPW1 is a potent and selective CDK9 inhibitor with excellent activity against clear cell renal cell carcinoma (ccRCC) and low toxicity .
|
-
-
- HY-103019A
-
(±)-BAY-1251152; (±)-VIP152
|
CDK
|
Cancer
|
(±)-Enitociclib ((±)-BAY-1251152) is a racemic mixture of BAY-1251152. BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.
|
-
-
- HY-111537
-
|
Others
|
Others
|
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-161379
-
|
CDK
|
Cancer
|
CLZX-205 (compound C-7) is a selective inhibitor of CDK9, with the IC50 of 2.9 nM. CLZX-205 plays an important role in cancer research .
|
-
-
- HY-12214A
-
NVP-2
Maximum Cited Publications
29 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-103019
-
(+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib
|
CDK
|
Cancer
|
(+)-Enitociclib ((+)-BAY-1251152) is an enanthiomer of BAY-1251152 with rotation (+). Enitociclib is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. Enitociclib has anti-tumour activity .
|
-
-
- HY-X0009
-
|
CDK
|
Others
Cancer
|
JSH-009 is a novel, highly selective CDK9 inhibitor critical for regulating transcription elongation. JSH-009 demonstrated significant in vitro and in vivo efficacy against acute myeloid leukemia (AML) .
|
-
-
- HY-111427
-
|
CDK
|
Cancer
|
CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC50s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.
|
-
-
- HY-X0009A
-
|
CDK
|
Cancer
|
JSH-009 dimaleate (Compound 1) is a potent and highly selective CDK9 inhibitor with an IC50 of 0.928 nM. JSH-009 can effectively inhibit the growth of subcutaneous tumor (cute myelogenous leukemia MV4-11) mice .
|
-
-
- HY-10008
-
BMS-387032
|
CDK
Apoptosis
|
Cancer
|
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 .
|
-
-
- HY-119120
-
|
HIV
CDK
|
Infection
Inflammation/Immunology
|
JTK-101 is a selective HIV inhibitor. JTK-101 selectively reduces HIV-1 mRNA synthesis by inhibiting Tat cofactors, including CDK9 and cyclin T1, thereby suppressing the transcriptional activity of HIV-1. JTK-101 may be used in the field of anti-HIV virus research .
|
-
-
- HY-145408
-
|
CDK
|
Cancer
|
CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC50s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer .
|
-
-
- HY-12422A
-
|
CDK
|
Cancer
|
Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL) .
|
-
-
- HY-12422
-
|
CDK
|
Cancer
|
Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL) .
|
-
-
- HY-162037
-
|
CDK
FLT3
|
Cancer
|
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
|
-
-
- HY-117203A
-
|
CDK
|
Cancer
|
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
|
-
-
- HY-108907
-
|
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-12843
-
|
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-116871
-
|
CDK
|
Cancer
|
YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
|
-
-
- HY-14372
-
|
CDK
|
Cancer
|
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer .
|
-
-
- HY-11009
-
|
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-103712A
-
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
-
- HY-103712B
-
CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrate
|
CDK
Apoptosis
|
Cancer
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
-
- HY-103712
-
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects .
|
-
- HY-103712C
-
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-138293
-
SY-5609
1 Publications Verification
CDK7-IN-3
|
CDK
Apoptosis
|
Cancer
|
SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity .
|
-
- HY-151878
-
|
CDK
GSK-3
|
Metabolic Disease
|
CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research .
|
-
- HY-149819
-
|
HDAC
CDK
|
Cancer
|
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
|
-
- HY-153221
-
|
CDK
|
Cancer
|
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer .
|
-
- HY-18944
-
|
CDK
HSV
CMV
DNA/RNA Synthesis
|
Infection
|
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.
|
-
- HY-103019E
-
BAY-1251152; VIP152
|
Others
|
Others
|
Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated. VIP152 shows promising long-term single-agent inhibitory activity against double-click refractory diffuse large B-cell lymphoma .
|
-
- HY-112371
-
|
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-110368
-
|
CDK
|
Cancer
|
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-13266
-
|
CDK
Apoptosis
|
Cancer
|
BS-181 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, 3000 and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 has the potential for the research of cancer therapy .
|
-
- HY-101257
-
|
CDK
|
Cancer
|
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
|
-
- HY-101257B
-
|
CDK
|
Cancer
|
YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
|
-
- HY-111388A
-
|
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 Kd 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-121081
-
|
CDK
|
Cancer
|
BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: