DTHIB |
Catalog No.GC62120 |
DTHIB는 HSF1 DNA 결합 도메인(DBD)에 결합하는 DTHIB의 Kd가 160nM인 직접적이고 선택적 열 충격 인자 1(HSF1) 억제제입니다. DTHIB는 HSF1 암 유전자 서명(HSF1 CaSig)을 억제하고 핵 HSF1의 분해를 선택적으로 자극합니다. DTHIB는 강력한 항암 활성을 가지며 전립선암 연구에 사용될 수 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 897326-30-6
Sample solution is provided at 25 µL, 10mM.
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research[1].
DTHIB (5 μM; 48 hours) treatment of C4-2 cells induces cell cycle arrest, with accumulation in the G1 phase. DTHIB stimulates C4-2 PCa cell entry into senescence[1]. DTHIB (0.5-5 μM; 48 hours; C4-2 prostate cancer) treatment reduces steady-state protein abundance of the molecular chaperones P23, HSP27, HSP70, and HSP90-all bona fide HSF1 targets in C4-2 cells[1]. DTHIB dose-dependently reduces the clonal expansion of both C4-2 and PC-3 PCa cells with EC50 values of 1.2 μM and 3.0 μM, respectively[1]. In mouse embryonic fibroblasts (MEFs), DTHIB (0.5-10 μM) attenuates the robust acute heat shock induction of the HSP70 and HSP25 molecular chaperones in a dose-dependent manner. DTHIB attenuates the heat shock response by reducing the steady-state transcript abundance of multiple molecular chaperones[1].
DTHIB (5 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment potently attenuates tumor progression in a C4-2 xenograft mouse model[1].
[1]. Bushu Dong, et al. Targeting therapy-resistant prostate cancer via a direct inhibitor of the human heat shock transcription factor 1. Sci Transl Med. 2020 Dec 16;12(574):eabb5647.
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(Based on Reviews and 34 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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