About 32 results found for searched term "CDK7-IN-1" (0.101 seconds)
Cat.No. | Name | Target |
---|---|---|
M41444 | CDK7-IN-21 | CDK |
CDK7-IN-21 is a potent CDK7 inhibitor. | ||
M57962 | CDK7-IN-1 | Others |
CDK7-IN-1 | ||
M1710 | Flavopiridol | CDK |
HMR-1275; Alvocidib; L86-8275 | ||
Flavopiridol (Alvocidib) is a competitive broad-spectrum CDK inhibitor with IC50 of 30,170,100 nM against CDK1, CDK2 and CDK4, respectively. | ||
M1800 | JNJ-7706621 | CDK |
JNJ7706621 | ||
JNJ-7706621 is a dual cell cycle inhibitor with activity against cyclin-dependent kinases (CDK1, 2, 3, 6) with an IC50 of 3-175 nM and Aurora kinases (A and B) with an IC50 of 11-15 nM respectively. | ||
M2434 | BAY 1000394 | CDK |
Roniciclib | ||
BAY 1000394 is an orally bioavailable pan-CDK inhibitor for CDK1/2/3/4/7/9 with IC50 of 5-25 nM. It also potently inhibits Aurora A, Clk2, ARK5, FGFR1, Flt3, and JAK2/3. Phase 1/2. | ||
M3504 | BS-181 hydrochloride | CDK |
BS-181 HCl | ||
BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. | ||
M5263 | LDC4297 | CDK |
LDC044297 | ||
LDC4297 is a novel CDK7 inhibitor (IC50=0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). | ||
M6160 | Bohemine | CDK |
Bohemine is A selective CDK inhibitor with IC50 of 4.6 μM, 83 μM and 2.7 μM against Cdk2/ Cyclin E, Cdk2/ Cyclin A and Cdk9/cyclin T1, respectively. Bohemine also inhibited ERK2, IC50 was 52 μM, and inhibited CDK1, CDK4 and CDK6. Bohemine is also a purine analogue and has a wide range of anticancer activities. | ||
M8995 | THZ2 | CDK |
THZ2 (an analog of THZ1) is a potent and selective CDK7 inhibitor which overcomes the instability of THZ1 in vivo (IC50s: CDK7=13.9 nM; TNBC cells=10 nM). | ||
M9489 | SY-1365 | CDK |
Mevociclib | ||
SY-1365 (Mevociclib) is a potent, first-in-class, selective CDK7 inhibitor with a Ki value of 17.4 nM.Mevociclib exhibits antiproliferative and apoptotic activity in solid tumor cell lines. | ||
M9910 | CDKI-73 | CDK |
CDKI73; Asnuciclib; LS-007 | ||
Cdki-73 (LS-007) is an orally active and highly effective CDK9 inhibitor with Ki values of 4 nM, 4 nM and 3 nM against CDK9, CDK1 and CDK2, respectively. Cdki-73 down-regulates phosphorylation of RNA polymerase II. Cdki-73 is also an inhibitor of Rab11. | ||
M10734 | YKL-5-124 | CDK |
YKL-5-124 is a potent, selective, irreversible COVALENT inhibitor of CDK7 and CDK7/Mat1/CycH IC50 53.5 nM and 9.7 nM, respectively. YKL-5-124 is more than 100 times more selective to CDK7 than CDK9 and CDK2 and is inactive to CDK12 and CDK13. YKL-5-124 induces intense cell cycle arrest and inhibits E2F-driven gene expression with little effect on RNA polymerase II phosphorylation status. | ||
M10843 | KB-0742 dihydrochloride | CDK |
KB-0742 dihydrochloride is a potent, selective and orally active CDK9 inhibitor against CDK9/cyclin T1 IC50 is 6 nM. KB-0742 dihydrochloride is selective for CDK9/cyclin T1, which is more than 50 times more selective than other CDK kinases. KB-0742 dihydrochloride has potent anti-tumor activity. | ||
M10886 | Samuraciclib hydrochloride | CDK |
Samuraciclib (ICEC0942, CT7001) is a novel oral CDK7 inhibitor with an IC50 of 40 nM. It has IC50 values for other CDK proteins such as CDK1, CDK2, CDK5 and CDK9 as 45, 15, 230 and 30 times higher than that of CDK7 IC50, respectively. ICEC0942 (CT7001) promotes cell cycle blocking and apoptosis. | ||
M10913 | THZ1-R | CDK |
THZ1-R is a non-cysteine-reactive analogue of THZ1 with reduced activity against CDK7 inhibition. THZ1-R in combination with CDK7 Kd 142 nM. | ||
M10966 | SY-5609 | CDK |
CDK7-IN-3 | ||
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). | ||
M13596 | Atuveciclib | CDK |
BAY-1143572 | ||
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. | ||
M13598 | BS-181 | CDK |
BS-181 is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib . | ||
M13617 | THZ1 Hydrochloride | CDK |
THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression. | ||
M13619 | YKL-5-124 TFA | CDK |
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. | ||
M21000 | LY3405105 | CDK |
LY3405105 is an orally active CDK7 inhibitor with an IC50 of 92.8 nM. LY3405105 shows potential antineoplastic activity. | ||
M21148 | (R)-CR8 trihydrochloride | CDK |
CR8, (R)-Isomer trihydrochloride | ||
(R)-CR8 trihydrochloride, one of the isomers of CR8, is a potent CDK1/2/5/7/9 inhibitor with anti-proliferative and pro-apoptotic effects on CML cell lines. (R)-CR8 trihydrochloride inhibited 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). | ||
M27775 | BS-194 | CDK |
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. | ||
M28894 | Samuraciclib | CDK |
CT7001; ICEC0942 | ||
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. | ||
M29110 | CDK12-IN-E9 | CDK |
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. | ||
M29440 | TL12-186 | PROTAC |
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). | ||
M29759 | SZ-015268 | CDK |
SZ-015268 is a CDK7 inhibitor with an IC50 of 23.56 nM. SZ-015268 has extremely significant anti-tumor advantages. SZ-015268 inhibits HCC70, OVCAR-3, HCT116 and HCC1806 cells proliferation with IC50s of 33, 80.56, 12.53, and 61.55 nM, respectively. | ||
M30608 | RGB-286147 | CDK |
RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity. | ||
M31194 | BS-181 dihydrochloride | CDK |
BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib. BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively. | ||
M31195 | CDK1/2/4-IN-1 | CDK |
CDK1/2/4-IN-1 is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. | ||
M31197 | CDK2/4/6-IN-1 | CDK |
CDK2/4/6-IN-1 is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. | ||
M41421 | ZNL-05-044 | CDK |
ZNL-05-044 is a CDK11 inhibitor with an IC50s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). |
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