KRIBB11


Catalog No. Size PriceQuantity
M12394-2 2mg solid $100
M12394-10 10mg solid $300

Description

KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.

Product information

CAS Number: 342639-96-7

Molecular Weight: 284.27

Formula: C13H12N6O2

Chemical Name: N2-(1H-indazol-5-yl)-N6-methyl-3-nitropyridine-2, 6-diamine

Smiles: CNC1=CC=C(C(NC2C=C3C=NNC3=CC=2)=N1)[N+]([O-])=O

InChiKey: NDJJEQIMIJJCLL-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 27 mg/mL (94.98 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

KRIBB11 blocks the induction of HSF1 downstream target proteins such as HSP27 and HSP70. KRIBB11 induces growth arrest and apoptosis of HCT-116 cells. KRIBB11 inhibits HSF1-dependent recruitment of p-TEFb (positive transcription elongation factor b) to the hsp70 promoter. PARP and caspase-3 cleavage is increased in cells treated with KRIBB11. Incubating RKO with KRIBB11, shows a toxic threshold of about 10 µM, and an IC50 of 20-30 µM.

In Vivo:

KRIBB11 (50 mg/kg, i.p.) results in a 47.4% inhibition of tumor growth in nude mice, without body weight loss.

References:

  1. Yoon YJ, et al. KRIBB11 inhibits HSP70 synthesis through inhibition of heat shock factor 1 function by impairing the recruitment of positive transcription elongation factor b to the hsp70 promoter. J Biol Chem. 2011 Jan 21;286(3):1737-47
  2. Samarasinghe B, et al. Heat shock factor 1 confers resistance to Hsp90 inhibitors through p62/SQSTM1 expression and promotion of autophagic flux. Biochem Pharmacol. 2014 Feb 1;87(3):445-55

Products are for research use only. Not for human use.

Payment & Security

American Express Diners Club Discover JCB Mastercard PayPal Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed