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KRIBB11 HSP (HSP90) inhibitor

Name: KRIBB11
Brand: Selleck Chemicals
SKU: S8402
Availability: InStock
Rating: 5 (14 reviews)

Cat.No.S8402

KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). This compound induces growth arrest and apoptosis.

Chemical Structure

Molecular Weight: 284.27

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.79%

99.79

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Chemical Information, Storage & Stability

Molecular Weight	284.27	Formula	C₁₃H₁₂N₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	342639-96-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CNC1=NC(=C(C=C1)[N+](=O)[O-])NC2=CC3=C(C=C2)NN=C3

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (351.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.470mg/ml (5.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 29.4 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.800mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 56 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	HSF1 ^[1] (Cell-based assay) 1.2 μM
In vitro	KRIBB11 inhibits HSF1 activity in a concentration-dependent manner. It down-regulates HSP70 and HSP27. This compound can inhibit cancer cell proliferation, arrests the cell cycle at G2/M phase and induces apoptosis. But it does not inhibit heat shock-induced recruitment of HSF1 to the hsp70 promoter or phosphorylation of HSF1 Ser-230. This chemical inhibits heat shock-induced recruitment of pTEFb to the hsp70 promoter and p-TEFb-dependent Phosphorylation of polⅡ CTD Ser-2^[1].
In vivo	Using a mouse xenograft model, KRIBB11 treatment decreases tumor volume by 47% compared with untreated control mice. In addition, HSP70 protein levels are significantly decreased in tumors from mice treated with this compound, supporting the notion that it exerts its in vivo antitumor activity through HSF1 inhibition^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/21078672/

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