protac cdk9 degrader-1

PROTAC CDK9 Degrader-1 is a selective PROTAC CDK9 degrader composed of a cereblon ligand and a CDK9 ligand.

PROTAC FLT3 CDK9 degrader-1, a potent dual degrader of FLT3 and CDK9, effectively induces apoptosis and targets protein degradation of FLT3 and CDK9. This compound holds research potential for FLT3-ITD mutated AML [1].

PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC CDK9 degrader with a DC50 of 1.09 nM. This compound exhibits cytotoxicity in small cell lung cancer (SCLC) cells, with IC50 values in the nanomolar range. It induces cell cycle arrest at the G0 G1 phase and inhibits cell invasion in DMS114 and DMS53 cells. In addition, PROTAC CDK9 degrader-11 shows antitumor activity in an NCI-H446 xenograft mouse model. (Pink: ligand for target protein CDK9 ligand 3; Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56)

CDK9-IN-11 is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 Degrader-1 [1].

PROTAC CDK2 9 Degrader-1 is a potent CDK2 and CDK9 dual degrader(DC50 of 62 nM and 33 nM).

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].

LC3B ligand 1 is the target protein ligand for PROTAC, and it can be utilized in the synthesis of PROTACCDK9 autophagic degrader 1.

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

PROTAC CDK9 degrader-5 is a selective PROTAC that mediates degradation of CDK9 via the proteasome pathway, efficiently degrading CDK9 42 and CDK9 55 isoforms with DC50 values of 0.10 μM and 0.14 μM, respectively [1].

PROTAC CDK9 degrader-6 is a specific PROTAC targeting CDK9 for degradation via the proteasome pathway, effectively degrading CDK9 with DC50 values of 0.10 μM and 0.14 μM for the CDK9 42 and CDK9 55 isoforms, respectively [1].

PROTAC CDK9 degrader-7 is a proteolysis-targeting chimera (PROTAC) engineered to selectively target and mediate the degradation of Cyclin-Dependent Kinase 9 (CDK9) via the proteasome pathway [1].

CP-07 is a selective and effective PROTAC CDK9 degrader (DC50: 43 nM), demonstrating inhibition of 22RV1 cell proliferation (IC50: 62 nM) and colony formation by attenuating levels of Mcl-1 and c-Myc. Additionally, CP-07 has been shown to impede the growth of 22RV1 xenograft tumors and is applicable in prostate cancer research [1].

PROTAC CDK9 Degrader-8 (Compound 21) is a potent degrader of CDK9 with an IC50 of 0.01 μM, utilized in cancer research [1].