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Chemical Structure : CT-189
Catalog No.: PC-49215Not For Human Use, Lab Use Only.
CT-189 (CT189) is a drug-like analog of IPAG and small-molecule Sigma1 receptor inhibitor, binds Sigma1 with Ki value of 38 nM in [3H](+)-pentazocine binding competition assays.
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CT-189 (CT189) is a drug-like analog of IPAG and small-molecule Sigma1 receptor inhibitor, binds Sigma1 with Ki value of 38 nM in [3H](+)-pentazocine binding competition assays.
CT-189 inhibits androgen receptor (AR) transcriptional activity and AR splice variant (ARV) signaling, decreases KLK3/PSA mRNA transcript levels in LNCaP cells and 22Rv1 cells, decreases levels of ARV7 as well as AR protein levels.
CT-189 prevents 5α-dihydrotestosterone (DHT)-mediated nuclear translocation of AR and induced proteasomal degradation of AR and ARV, suppressing the transcriptional activity and protein levels of both full-length and splice-variant AR.
CT-189 (30 mg/kg, oral gavage) inhibits the growth of xenografted 22Rv1 tumors by 60% following -36 days of treatment.
| M.Wt | 321.780 | |
| Formula | C16H17ClFN3O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jeffrey D. Thomas, et al. Cancer Res. 2017 May 1; 77(9): 2439–2452.
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