| DC55130 |
CDK4 inhibitor compound 12
|
CDK4 inhibitor compound 12 is a novel inhibitor of CDK4 with the activity 97 μM. |
| DC28035 |
TCMDC-135051
|
TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM). |
| DC27001 |
SR-4835
|
SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13. |
| DC73170 |
GFH009
|
GFH009 is a potent, selective CDK9 inhibitor, inhibits the activity of the CDK9/cyclin T1 regulatory complex of P-TEFb. |
| DC70984 |
(S)-CR8
|
(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). |
| DC70766 |
Senexin C
|
Senexin C is a novel potent, selective and orally bioavailable CDK8/19 inhibitor with Kd of 1.4 and 2.9 nM for CDK8/CycC and CDK19/CycC, respectively.Senexin C inhibits CDK8/CycC with IC50 of 3.6 nM, shows high selectivity against other HDAC isoforms.Senexin C is more metabolically stable and provides a more sustained inhibition of CDK8/19-dependent cellular gene expression when compared with the prototype inhibitor Senexin B.Senexin C inhibits MV4-11 leukemia growth in a systemic in vivo model with good tolerability. |
| DC70595 |
MFH290
|
MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib. |
| DC70298 |
CDDD11-8
|
CDDD11-8 is a potent CDK9 inhibitor co-targeting FLT3-ITD with Ki values of 8 and 13 nM, respectively.CDDD11-8 displays excellent kinome selectivity in a panel of 369 human kinases.CDDD11-8 displays antiproliferative activity against leukemia cell lines, and particularly potent effects against MV4-11 and MOLM-13 cells, which are known to harbor the FLT3-ITD mutation and mixed lineage leukemia (MLL) fusion proteins.CDDD11-8 causes a robust tumor growth inhibition by oral administration in animal xenografts, induces tumor regression at dose of 125 mg/kg. |
| DC70230 |
AZ5576
|
AZ5576 (AZ-5576) is a potent, selective CDK9 inhibitor with an IC 50 <5 nM, decreases phosphorlyation of Ser2-RNAPII in cells with an IC 50 of 96 nM.AZ5576 downregulated Mcl-1 and MYC protein abundance across multiple tested DLBCL cell lines and in primary DLBCL cells.MYC sensitizes DLBCL cells to AZ5576, genetic downregulation of MYC in U-2932 and OCI-LY19 cells resulted in diminished susceptibility to AZ5576.AZ5576 dose-dependently downregulated MYC transcription of a luciferase reporter containing multiple canonical MYC-MAX-binding sites, an effect more pronounced compared with multi-CDK inhibitor dinaciclib.AZ5576 restricts growth of xenografted DLBCL tumors in vivo. |
| DC70109 |
(R)-CR8
|
(R)-CR8 is a potent CDK1/2/5/7/9 inhibitor, inhibits CDK1/cyclin B (IC50, 90 nM), CDK2/cyclin A (72 nM), CDK2/cyclin E (41 nM), CDK5/p25 ( 110 nM), CDK7/cyclin H (1.1 uM), CDK9/cyclin T (0.18 uM) and CK1δ/ε (0.4 uM);
(R)-CR8 induces apoptosis and has neuroprotective effect, CR8 alsp acts as a molecular glue degrader that depletes cyclin K. |
