DTHIB

Catalog No.S9806 Batch:S980601

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Technical Data

Formula

C13H9ClFN3O3
Molecular Weight 309.68 CAS No. 897326-30-6
Solubility (25°C)* In vitro DMSO 86 mg/mL (277.7 mM)
Ethanol 17 mg/mL (54.89 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities.
Targets
HSF1 [1]
(Cell-free assay)
160 nM(Kd)
In vitro

Direct Targeted HSF1 InhiBitor (DTHIB) physically engages HSF1 and selectively stimulates degradation of nuclear HSF1. DTHIB robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.[1]
In vivo

DTHIB potently attenuates tumor progression in four therapy-resistant prostate cancer animal models, including an NEPC model, where it causes profound tumor regression.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    C4-2, PC-3, BPH-1 cells

  • Concentrations

    0.5 μM, 1.0 μM, 2.5 μM, 5 μM

  • Incubation Time

    36-hour, 48-hour, 96-hour

  • Method

    C4-2 Scr and shHSF1 cells exposed to 36-hour treatment with 2.5 μM DTHIB are evaluated for HSF1 target gene expression by qRT-PCR.
Animal Study:

[1]
  • Animal Models

    6-week-old nude (nu/nu) mice; 6 week-old C57BL/6 mice

  • Dosages

    1 mg/kg, 5 mg/kg

  • Administration

    IP

Selleck's DTHIB has been cited by 1 publication

Increased mitochondria are responsible for the acquisition of gemcitabine resistance in pancreatic cancer cell lines [ Cancer Sci, 2023, 114(11):4388-4400.] PubMed: 37700464

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.