Home Cytoskeletal Signaling HSP (HSP90) inhibitor DTHIB For research use only.

DTHIB

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.

DTHIB Chemical Structure

DTHIB Chemical Structure

CAS: 897326-30-6

Selleck's DTHIB has been cited by 1 publication

Purity & Quality Control

Batch: S980601 DMSO] 86 mg/mL] false] Ethanol] 17 mg/mL] false] Water] Insoluble] false Purity: 99.76%
99.76

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 6-week-old nude (nu/nu) mice; 6 week-old C57BL/6 mice
Dosages 1 mg/kg, 5 mg/kg
Administration IP

Chemical lnformation & Solubility

Molecular Weight 309.68 Formula

C13H9ClFN3O3
CAS No. 897326-30-6 SDF --
Smiles [O-][N+](=O)C1=CC(=CC=C1Cl)NC(=O)NC2=CC=C(F)C=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 86 mg/mL ( (277.7 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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