385570
Heat Shock Factor 1 Inhibitor, KRIBB11
The Heat Shock Factor 1 Inhibitor, KRIBB11 controls the biological activity of Heat Shock Factor 1.
동의어(들):
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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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C13H12N6O2
CAS 번호:
Molecular Weight:
284.27
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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
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.
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.
Other Notes
Yoon, Y.J., et al. 2010. J. Biol. Chem.286, 1737.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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.
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국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 385570-10MGCN | 04055977190274 |
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