CSRM617

CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model[1]

Product Specifications

CAS Number

[787504-88-5]

UNSPSC

12352005

Target

Androgen Receptor; Apoptosis

Type

Reference compound

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/csrm617.html

Solubility

10 mM in DMSO

Smiles

O=C(C(CO)N)N/N=C/C1=CC=C(C(O)=C1O)O

Molecular Formula

C10H13N3O5

Molecular Weight

255.23

References & Citations

[1]Rotinen M, et al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24 (12) :1887-1898.