DTHIB

SKU: orb1217517

Description

DTHIB robustly inhibits the HSF1 cancer gene signature and prostate cancer cell proliferation.

Images & Validation

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Key Properties

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CAS Number	897326-30-6
MW	309.68
Purity	>98% (HPLC)
Formula	C₁₃H₉ClFN₃O₃
SMILES	O=C(NC1=CC=C(F)C=C1)NC2=CC=C(Cl)C([N+]([O-])=O)=C2
Target	HSP
Solubility	DMSO:10 mM

Bioactivity

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In Vivo

DTHIB (5 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment potently attenuates tumor progression in a C4-2 xenograft mouse model. Animal model: Nude mice (6 weeks of age) injected with C4-2 cells. Dosage: 5 mg/kg. Administration: Intraperitoneal injection; daily; for 3 weeks. Result: Showed no visible tumor growth over a 3-week period and a 40% reduction in median tumor volume.

In Vitro

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. 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. 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. 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. Cell Cycle Analysis Cell line: C4-2 cells. Concentration: 5 μM. Incubation time: 48 hours. Result: Induced cell cycle arrest. Western blot analysis. Cell line: C4-2 prostate cancer (PCa) cells. Concentration: 0.5 μM, 1 μM, 2.5 μM, 5 μM Incubation time: 48 hours. Result: Dose-dependently inhibited expression of molecular chaperones in C4-2 PCa cells.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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HSP

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DTHIB (orb1217517)

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Purity:	99.69% (May vary between batches)
CAS Number:	897326-30-6
MW:	309.68
Formula:	C₁₃H₉ClFN₃O₃

DTHIB

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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DTHIB (orb1217517)

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