Cas No.: | 787504-88-5 |
Chemical Name: | 2-amino-3-hydroxy-N'-(2,3,4-trihydroxybenzylidene)propanehydrazide |
Synonyms: | CSRM-617;CSRM 617 |
SMILES: | C(N/N=C/C1=CC=C(O)C(O)=C1O)(=O)C(N)CO |
Formula: | C10H13N3O5 |
M.Wt: | 255.23 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [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. |
Description: | CSRM617 (CSRM-617) is a small-molecule inhibitor of the transcription factor ONECUT2 (OC2) with Kd of 7.43 uM in SPR assays, binds to OC2-HOX domain directly; inhibits cell growth and induced apoptosis in vitro in several PC cell lines that expressed moderate to high levels of OC2; significantly downregulates PEG10 protein levels in tumors from mice treated with CSRM617, suppresseses metastasis in 22Rv1 cells implanted subcutaneously nude mice. |
In Vitro: | CSRM617 (0.01-100 μM; 48 hours) inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells[1]. CSRM617 (10-20 μM; 48 hours) induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion[1]. CSRM617 (20 μM; 72 hours) induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP[1]. |
References: | [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. |