HSF1A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子人类 HSF1（热休克转录因子 1）激活剂。

A small molecule human HSF1 (heat shock transcription factor 1) activator; activates HSF1 in mammalian and fly cells, elevates protein chaperone expression, ameliorates protein misfolding and cell death in polyQ-expressing neuronal precursor cells and protects against cytotoxicity in a fly model of polyQ-mediated neurodegeneration; also interacts with components of the TRiC/CCT complex.

HSF1A protects cells from stress-induced apoptosis, binds TRiC subunits and inhibits TRiC activity without perturbation of ATP hydrolysis. Genetic inactivation or depletion of the TRiC complex results in human HSF1 activation and HSF1A inhibits the direct interaction between purified TRiC and HSF1 in vitro. Moreover, fluorescence anisotropy experiments using FITC coupled to HSF1A demonstrates that HSF1A-FITC binds to a purified Tcp1 subunit of TRiC with an affinity of approximately 600 nM. This is validated qualitatively via titration of purified Tcp1 into binding reactions containing 500 nM Biotin or HSF1A-Biotin. Quantification by counting the number of cell containing aggregates as a function of the total number of cells reveals that at HSF1A concentrations as low as 2 μM, a reduced number of aggregate-containing cells are observed. The fraction of cells containing aggregates continued to decrease in a dose-dependent manner such that pretreatment with 12 μM HSF1A resulta in ~20% of the cells exhibiting aggregates visible by fluorescence microscopy.

HSF1A enhances HSF1 activity, stabilizes HSF1 expression and minimizes Doxorubicin (DOX)-induced cardiac damage.WKY rats are challenged with DOX (accumulated dose: 30?mg/kgw), and DOX combined with HSF1A (100?mg/kgw/day). Supplementation with HSF1A significantly elevates cardiac functions back to the levels of the control group. HSF1A has been shown to stimulate human HSF1 nuclear translocation, elevate protein chaperone expression and ameliorate protein misfolding and cell death in a neurodegenerative disease model. The echocardiographic results show that HSF1A also alleviates DOX-induced failures in cardiac function.

HSF1 activator

Cytoskeleton/Cell Adhesion Molecules

HSP

HSF1

Other Indications

——

1196723-93-9

409.522

C21H19N3O2S2

>98% (HPLC)

DMSO: ≥150 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=S(C1=CC=C(CC)C=C1)(NC2=CC(C3=CC=CS3)=NN2C4=CC=CC=C4)=O

4-ethyl-N-(1-phenyl-3-(thiophen-2-yl)-1H-pyrazol-5-yl)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years