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KY-226 phosphatase inhibitor

Name: KY-226
Brand: Selleck Chemicals
SKU: S0136
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S0136

KY-226 is a potent, selective, orally active and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 μM for human PTP1B activity. This compound exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively.

Chemical Structure

Molecular Weight: 481.67

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

Quality Control

Batch: S013601 DMSO]96 mg/mL]false]Ethanol]1.5 mg/mL]false]Water]Insoluble]false Purity: 99.7%

99.7

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Chemical Information, Storage & Stability

Molecular Weight	481.67	Formula	C₂₇H₃₁NO₃S₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1621673-53-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCCCCCS(=O)(=O)NC(=O)C1=CC=C(C=C1)CSCC2=CC=C(C=C2)C3=CC=CC=C3

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (199.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1.5 mg/mL

Water : 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.	4.8mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 96 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.	0.67mg/ml (1.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.4 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.

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	PTP1B ^[1] (Cell-free assay) 0.28 μM
In vitro	KY-226 inhibits human PTP1B activity, but does not exhibit peroxisome proliferator-activated receptor γ (PPARγ) agonist activity. In rodent preadipocytes (3T3-L1), this compound up to 10 μM has no effects on adipocyte differentiation. In human hepatoma-derived cells (HepG2), this chemical (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin.^[1]
In vivo	In db/db mice, the oral administration of KY-226 (10 and 30 mg/kg/day, 4 weeks) significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain. This compound attenuates plasma glucose elevations in the oral glucose tolerance test. It also increases pIR and phosphorylated Akt in the liver and femoral muscle. In high-fat diet-induced obese mice, the oral administration of this chemical (30 and 60 mg/kg/day, 4 weeks) decreases body weight gain, food consumption, and fat volume gain with increases in phosphorylated STAT3 in the hypothalamus.^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/29731242/

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