CDK7 inhibitor

THZ1 (CDK7 inhibitor) is a selective covalent inhibitor of CDK7, exhibiting binding affinity to the cysteine residue located at the outer end of the classical kinase domain, thus conferring high selectivity for CDK7, with an IC50 of 3.2 nM.

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.

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

SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor (Kd value is 0.07 nM), with weak inhibitory activity against CDK2, CDK9 and CDK12 with IC50 values ​​of 5.5, 1.9 and 1.7 μM, respectively, and has anti-tumor activity and inhibits cell apoptosis.

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.

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.

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

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.

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).

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

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

bio-THZ1 is a biotinylated version of THZ1, a selective and irreversibly covalent CDK7 inhibitor (IC50: 3.2 nM).

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective CDK4/CDK6 inhibitor, with IC50 values of 2 nM for CDK6/CyclinD3 and 1 nM for CDK4/CyclinD1.

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

YKL-5-124 TFA is a potent, selective, irreversible and covalent inhibitor of CDK7 (IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7 Mat1 CycH, respectively).

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

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.

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.

Roniciclib (BAY 1000394) is a potent pan-CDK inhibitor and a novel oral cytotoxic agent. Roniciclib inhibits the activity of cell-cycle CDKs CDK1, CDK2, CDK3, CDK4, and of transcriptional CDKs CDK7 and CDK9 with IC(50) values in the range between 5 and 25 nmol L.

CDK7-IN-31 (compound 13) is an effective and orally active inhibitor of cyclin-dependent kinase 7 (CDK7) with a dissociation constant (Kd) of 0.18 nM. This compound exhibits anticancer activity.

TMX-2039 is a pan-CDK inhibitor that targets cell cycle CDKs (CDK1, CDK2, CDK4, CDK5, and CDK6) and transcription CDKs (CDK7 and CDK9), with IC50 values of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5, and 25 nM, respectively. It serves as a ligand for the target protein in PROTAC applications.

CDK7-IN-32 (compound10) is an inhibitor of CDK7.

CDK7-IN-33 (Compound 148) is a CDK7 inhibitor with a Ki value of 21.75 nM. It suppresses the proliferation of A549 cells expressing CDK7WT, with a pIC50 of 7.37.

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.