cdk7

CDK7-IN-7, a highly potent and selective inhibitor of CDK7 kinase, exhibits remarkable activity with an IC50 of less than 50 nM.

SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis.

CDK7-IN-16 (Compound 9) is a potent inhibitor of CDK 7 (IC50: 1-10 nM). CDK7-IN-16 can be used in research against cancer, particularly cancers with transcriptional abnormalities.

CDK7-IN-5, a CDK7 inhibitor with an IC 50 value of less than 100 nM, exhibits potent anticancer properties (WO2015154022A1, Compound 104).

CDK7-IN-13 is a pyrimidine-derived compound that is a potent inhibitor of CDK7. CDK7-IN-13 has the potential to be investigated in a variety of cancers (particularly those with dysregulated transcription).

CDK7 9 tide is a peptide substrate for CDK7 or CDK9[1].

CDK7-IN-20 is a potent, selective, and irreversible inhibitor of Cyclin-Dependent Kinase 7 (CDK7) with an IC50 value of 4 nM, exhibiting over 206-fold selectivity against related kinases [CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12]. It holds potential for research into autosomal dominant polycystic kidney disease (ADPKD).

CDK7-IN-17 is a pyrimidine-derived compound and a potent inhibitor of CDK7. CDK7-IN-17 has shown research potential for a variety of cancers, particularly those with dysregulated transcription.

CDK7-IN-2 is a potent inhibitor of CDK7, which plays a role in transcription initiation via phosphorylation of the Rbpl subunit of RNA polymerase II (RNAPII). CDK7 is linked to the temporal control of the cell cycle and transcriptional activity, and has research potential for aggressive and difficult-to-treat cancers.

CDK7-IN-10 is a CDK7 inhibitor (IC50 < 100 nM) that inhibits kinase activity, with potential to impede cell growth and induce apoptosis.

CDK7-IN-2 hydrochloride hydrate (Example 6) is a potent and specific inhibitor of the CDK7 enzyme, exhibiting significant anti-cancer properties.

CDK7-IN-25 (CY-16-1) is a highly potent CDK7 inhibitor with an IC50 of less than 1nM, used in cancer research [1].

CDK7-IN-15 is a pyrimidine-derived compound and a potent inhibitor of CDK7. CDK7-IN-15 has the potential to be investigated in a variety of cancers, particularly those with dysregulated transcription.

CDK7-IN-21 (compound A22) is a potent inhibitor of CDK7 [1].

CDK7 12-IN-1 is a selective inhibitor of CDK7 (IC50: 3 nM) and CDK12 (IC50: 277 nM) and effectively inhibits tumor growth.

CDK7 9-IN-1 is a specific inhibitor of cyclin-dependent kinases 7 9 (CDK7 9), targeting CDK7 with IC50 values of 0.0656 μM without pre-incubation and 0.00574 μM after 3 hours pre-incubation, and displaying inhibitory activity against CDK9 with an IC50 of 2.14 μM after 3 hours pre-incubation, making it valuable for cancer research.

CDK7-IN-12 is an effective CDK7 inhibitor and plays a key role in regulating transcription and cell cycle. CDK7-IN-12 can effectively inhibit the proliferation of malignant tumors in vitro and in vivo. CDK7-IN-12 has research potential in cancer diseases.

CDK7-IN-18 is a pyrimidine-derived compound that is a potent inhibitor of CDK7. CDK7-IN-18 exhibits potential for research in a variety of cancers, particularly those with dysregulated transcription.

CDK7-IN-14 is a pyrimidine-derived compound that is a potent inhibitor of CDK7. CDK7-IN-14 has the potential to be investigated in a variety of cancers, particularly those with transcriptional dysregulation.

CDK7-IN-1 is an analog derived from YKL-5-124 and functions as an inhibitor of cyclin-dependent kinase 7 (cdk7). It exhibits strong inhibitory activity, with an IC50 value of less than 100 nM (WO 2016105528 A2, Compound 215).

CDK7-IN-8, a potent inhibitor of CDK7 (IC50: 54.29 nM), demonstrates inhibitory activity against several cancer cells and in vivo tumor models.

CDK7-IN-22 (compound 101) is a selective CDK7 inhibitor with demonstrated antitumor activity and specificity for CDK7 [1].

CDK7-IN-6 is a highly effective and specific inhibitor (IC50 ≤100 nM) of cyclin-dependent kinase 7 (CDK7). It showcases remarkable selectivity, with more than a 200-fold preference for CDK7 over CDK1, CDK2, and CDK5. This compound holds significant potential for cancer research purposes.

HDAC1 CDK7-IN-1 (compound 8e) is a dual inhibitor of CDK7 and HDAC1, with IC50 values of 893 nM and 248 nM, respectively. It suppresses the proliferation of cancer cell lines such as MDA-MB-231, MCF-7, A549, and HCT-116, induces cell cycle arrest and apoptosis in HCT-116 cells, and impedes their migration [1].

THZ1 (CDK7 inhibitor) is a novel selective and potent covalent CDK7 inhibitor.

THZ2 (CDK7-IN-1), an analog of THZ1, is a potent and selective CDK7 inhibitor(IC50:13.9 nM),with the potential to treat Triple-negative breast cancer (TNBC).

LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.

LDC3140 is a potent inhibitor of Cyclin-dependent kinase 7 (CDK7).

R547 (Ro 4584820) is a potent ATP-competitive inhibitor of CDK1 2 4 with Ki of 2 nM 3 nM 1 nM. It is less potent to CDK7 and GSK3α β, while inactive to other kinases. Phase 1.

NVP-LCQ195 (LCQ-195) (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1 2 3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1 2.

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1 2 4 5 6 9.

AT7519 is a CDK1 2 4 6 9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

Seliciclib (Roscovitine) is a potent inhibitor of Cdk2 cyclin E (IC50=0.1 µM). Seliciclib also inhibits Cdk7 cyclin H, Cdk5 p35 and Cdc2 cyclin B (IC50=0.49 0.16 0.65 µM). Seliciclib has antitumor activity.

PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors.

SNS-032 (BMS-387032) is a selective inhibitor of CDK2 (IC50: 48 nM), exhibiting 10- and 20-fold selectivity over CDK1 and CDK4, respectively. It is also sensitive to CDK7 (IC50: 62 nM) and CDK9 (IC50: 4 nM), with no effect on CDK6.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 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.

TP-353 (EOS-61973) is a CDK7 inhibitor.

NU6140 is a selective inhibitor of CDK2-cyclin A (IC50, 0.41 μM). It shows 10- to 36-fold selectivity over other CDKs. NU6140 also effectively inhibits Aurora A and Aurora B (IC50s: 67 and 35 nM, respectively). It also enhances the apoptotic effect and has anti-cancer activity.

(R)-CR8 ((R)-Isomer) is a potent and selective CDK inhibitor.

LY2857785 is a type I competitive and reversible ATP kinase inhibitor against CDK7 CDK8 CDK9 (IC50s: 246 nM 16 nM 11 nM).

LY3405105 (1-Piperidinecarboxylic acid, 4-[[5-methyl-3-(1-methylethyl)pyrazolo[1,5-a]pyrimidin-7-yl]amino]-, 1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-3-pyrrolidinyl ester) is a novel CDK7 inhibitors.

Longdaysin is an inhibitor of CK1α and CK1δ (IC50s: 5.6 8.8 µM). It also can inhibit ERK2 (IC50: 52 µM).

SHR5428 is an orally active, selective, noncovalent inhibitor of CDK7, displaying potent enzymatic inhibition (IC50 = 2.3 nM) and effectively suppressing cellular activity in triple-negative breast cancer MDA-MB-468 cells (IC50 = 6.6 nM) [1].

CGP60474 is an inhibitor of VEGFR-2 (IC50 = 84 nM) and an inhibitor of ATP-competitive PKC. CGP60474 is also a highly potent anti-endotoxemic agent and inhibits cyclin-dependent kinase (CDK) potently.

Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive, orally active inhibitor of CDK7 (IC50: 41 nM). It inhibits the growth of breast cancer cell lines (GI50: 0.2-0.3 μM) and exhibits potent antitumor effects.

YKL-5-124 TFA, a potent and selective irreversible covalent inhibitor of CDK7, demonstrates IC50 values of 53.5 nM for CDK7 and 9.7 nM for the CDK7/Mat1/CycH complex. It exhibits over 100-fold selectivity for CDK7 over CDK9 and CDK2, while showing no activity against CDK12 and CDK13. This compound effectively induces cell-cycle arrest, inhibits E2F-driven gene expression, and has minimal impact on the phosphorylation status of RNA polymerase II.

GFB-12811 is a highly selective and orally active inhibitor of cyclin-dependent kinase 5 (CDK5), exhibiting an inhibitory concentration (IC50) of 2.3 nM. It demonstrates notable specificity, with minimal activity against other tested kinases, including CDK1, CDK2, CDK6, CDK7, and CDK9 [1].

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7, possessing therapeutic potential in both hematological and solid tumors.