DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM. DTHIB physically engages HSF1 and selectively stimulates degradation of nuclear HSF1. DTHIB robustly inhibited the HSF1 cancer gene signature and prostate cancer cell proliferation. In addition, it potently attenuated tumor progression in four therapy-resistant prostate cancer animal models, including an NEPC model, where it caused profound tumor regression.
MedKoo Cat#: 555912
Name: DTHIB
CAS#: 897326-30-6
Chemical Formula: C13H9ClFN3O3
Exact Mass: 309.0316
Molecular Weight: 309.68
Elemental Analysis: C, 50.42; H, 2.93; Cl, 11.45; F, 6.13; N, 13.57; O, 15.50
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMSO | 93.0 | 300.31 | |
Ethanol | 17.0 | 54.90 |
The following data is based on the product molecular weight 309.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |