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Merck

385570

Heat Shock Factor 1 Inhibitor, KRIBB11

The Heat Shock Factor 1 Inhibitor, KRIBB11 controls the biological activity of Heat Shock Factor 1.

Sinónimos:

Heat Shock Factor 1 Inhibitor, KRIBB11, Hsp70 Induction Inhibitor II, N²-(1H-Indazol-5-yl)-N⁶-methyl-3-nitropyridine-2,6-diamine, HSF1 Inhibitor, KRIBB11, Heat Shock Protein Inhibitor III, p-TEFb hsp70 Promoter Recruitment Inhibitor

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C13H12N6O2
Número CAS:
342639-96-7
Peso molecular:
284.27
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD30182306

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Nombre del producto

Heat Shock Factor 1 Inhibitor, KRIBB11, The Heat Shock Factor 1 Inhibitor, KRIBB11 controls the biological activity of Heat Shock Factor 1.

InChI

1S/C13H12N6O2/c1-14-12-5-4-11(19(20)21)13(17-12)16-9-2-3-10-8(6-9)7-15-18-10/h2-7H,1H3,(H,15,18)(H2,14,16,17)

InChI key

NDJJEQIMIJJCLL-UHFFFAOYSA-N

SMILES string

CNC(C=C1)=NC(NC2=CC3=C(NN=C3)C=C2)=C1[N+]([O-])=O

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange-yellow

solubility

DMSO: 50 mg/mL, brown

shipped in

ambient

storage temp.

−20°C

Quality Level

200

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable 2,6-diaminopyridine compound that interacts with HSF1 (heat shock factor 1) in a reversible manner and prevents HSF1 from recruiting p-TEFb (positive transcription elongation factor b) to the hsp70 promoter site (IC50 ≤3 µM in HCT-116 ChIP assays), a critical step for the p-TEFb CDK9 subunit-catalyzed pol II CTD (RNA polymerase II c-terminal domain) Ser-2 phosphorylation and transcription activation upon heat shock induction (IC50<1, <3, <5, and <10 µM, respectively, against reporter, HSP47, HSP27, and HSP70 transcription in HCT-116 cultures). Reported to exhibit antiproliferation activity against several cancer cultures in vitro (IC50 ranges from 3 to 8 µM) and effectively suppress HCT-116-derived tumor growth in mice in vivo (by 47.4% on day 31; single i.p. dosage of 50 mg/kg on day 13 after cancer implantation). Does not affect TNF-α-induced NF-κB activity in HeLa or heat shock-induced HSF1 ser230 phosphorylation and promoter association in HCT-116 even at concentrations as high as 10 µM.

Other Notes

Yoon, Y.J., et al. 2010. J. Biol. Chem.286, 1737.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Young Ju Yoon et al.
The Journal of biological chemistry, 286(3), 1737-1747 (2010-11-17)
Heat shock factor 1 (HSF1) is the master switch for heat shock protein (HSP) expression in eukaryotes. A synthetic chemical library was screened to identify inhibitors of HSF1 using a luciferase reporter under the control of a heat shock element.
Lea Danics et al.
Cancers, 12(9) (2020-09-16)
Modulated electro-hyperthermia (mEHT) is a complementary antitumor therapy applying capacitive radiofrequency at 13.56 MHz. Here we tested the efficiency of mEHT treatment in a BALB/c mouse isograft model using the firefly luciferase-transfected triple-negative breast cancer cell line, 4T1. Tumors inoculated
Maruhen Ad Silveira et al.
Life science alliance, 4(5) (2021-02-18)
Master transcription factors control the transcriptional program and are essential to maintain cellular functions. Among them, steroid nuclear receptors, such as the estrogen receptor α (ERα), are central to the etiology of hormone-dependent cancers which are accordingly treated with corresponding
Sara C Sebag et al.
Cell reports, 37(7), 110003-110003 (2021-11-18)
Brown adipose tissue (BAT) thermogenic activity is tightly regulated by cellular redox status, but the underlying molecular mechanisms are incompletely understood. Protein S-nitrosylation, the nitric-oxide-mediated cysteine thiol protein modification, plays important roles in cellular redox regulation. Here we show that
Greg A Timblin et al.
Nature metabolism, 3(5), 618-635 (2021-05-26)
Macrophages generate mitochondrial reactive oxygen species and mitochondrial reactive electrophilic species as antimicrobials during Toll-like receptor (TLR)-dependent inflammatory responses. Whether mitochondrial stress caused by these molecules impacts macrophage function is unknown. Here, we demonstrate that both pharmacologically driven and lipopolysaccharide

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