Home Metabolism phosphatase inhibitor KY-226 For research use only.

KY-226

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. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively.

KY-226 Chemical Structure

KY-226 Chemical Structure

CAS No. 1621673-53-7

Purity & 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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Biological Activity

Description 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. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively.
Targets
PTP1B [1]
(Cell-free assay)
0.28 μM
In vitro
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), KY-226 up to 10 μM has no effects on adipocyte differentiation. In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin.[1]
Cell Research Cell lines 3T3-L1, HepG2
Concentrations 0.1-10 μM
Incubation Time 1 h
Method

Cells with or without the overexpression of PTP1B are seeded at a density of 1 x 10 cells/well on 6-well plates and cultured for 24 h and then for 6 h in serumfree DMEM. Cells are cultured in the presence or absence of KY226 for 1 h, followed by an incubation with insulin for 10 min.Cells are washed and then used for various assays.
In Vivo
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. KY-226 attenuates plasma glucose elevations in the oral glucose tolerance test. KY-226 also increases pIR and phosphorylated Akt in the liver and femoral muscle. In high-fat diet-induced obese mice, the oral administration of KY-226 (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]

Chemical Information & Solubility

Molecular Weight 481.67 Formula

C27H31NO3S2
CAS No. 1621673-53-7 SDF --
Smiles CCCCCCS(=O)(=O)NC(=O)C1=CC=C(C=C1)CSCC2=CC=C(C=C2)C3=CC=CC=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (199.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1.5 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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