1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. KY-226

KY-226 

Cat. No.: HY-120327 Purity: 98.02%
Handling Instructions

KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.

For research use only. We do not sell to patients.

KY-226 Chemical Structure

KY-226 Chemical Structure

CAS No. : 1621673-53-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 159 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
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10 mg USD 250 In-stock
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25 mg USD 450 In-stock
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50 mg USD 750 In-stock
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100 mg USD 1100 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury[1][2].

IC50 & Target

IC50: 0.25 μM (Protein tyrosine phosphatase 1B (PTP1B))[2]

In Vitro

In human hepatoma-derived cells (HepG2), KY-226 (0.3-10 μM) increases the phosphorylated insulin receptor (pIR) produced by insulin[1].
KY-226 (1 μM; 24 hours; bEnd.3 cells) treatment rescues lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1. KY-226 treatment restores phosphorylation of pAkt (T308) and its downstream target forkhead box protein O1 (FoxO1) (S256) in bEnd.3 cells[2].

Western Blot Analysis[1]

Cell Line: bEnd.3 cells stimulated with LPS
Concentration: 1 μM
Incubation Time: 24 hours
Result: Rescued lipopolysaccharide-induced reduction of mRNA and protein levels of ZO-1.
In Vivo

KY-226 (10-30 mg/kg/day; oral administration; daily; for 4 weeks; male db/db mice) treatment significantly reduces plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain[1].
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[1].

Animal Model: Male db/db mice (8-11 weeks old)[1]
Dosage: 10 mg/kg and 30 mg/kg
Administration: Oral administration; daily; for 4 weeks
Result: Significantly reduced plasma glucose and triglyceride levels as well as hemoglobin A1c values without increasing body weight gain.
Molecular Weight

481.67

Formula

C₂₇H₃₁NO₃S₂

CAS No.

1621673-53-7

SMILES

O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (519.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0761 mL 10.3806 mL 20.7611 mL
5 mM 0.4152 mL 2.0761 mL 4.1522 mL
10 mM 0.2076 mL 1.0381 mL 2.0761 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

KY-226KY226KY 226PhosphatasePTP1Banti-diabeticanti-obesityinsulinleptinphosphorylatedAktZO-1neuronsLPSInhibitorinhibitorinhibit

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KY-226
Cat. No.:
HY-120327
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