KY-226

Alias: KY-226 KY 226 KY226
Cat No.:V34665 Purity: ≥98%
KY-226 is a novel, selective, orally bioactive and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with anIC50of 0.25 μM, and without PPARγ agonist activity.
KY-226 Chemical Structure CAS No.: 1621673-53-7
Product category: Phospholipase
This product is for research use only, not for human use. We do not sell to patients.
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Product Description

KY-226 is a novel, selective, orally bioactive and allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) 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. KY-226 protects neurons from cerebral ischemic injury. KY-226 restores Akt (protein kinase B) phosphorylation and extracellular signal-regulated kinase (ERK) reduction in transient middle cerebral artery occlusion (tMCAO) damage. KY-226 protects BBB integrity by restoration of TJ proteins, an effect partly mediated by Akt/FoxO1 pathway activation.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In human Manhattan-derived cells (HepG2), KY-226 (0.3-10 μM) enhances insulin synthesis at the phosphorylated insulin receptor (pIR) [1]. The reductions in ZO-1 mRNA and protein levels caused by LPS were reversed by treatment with KY-226 (1 μM; 24 hours; bEnd.3 cells). pAkt (T308) and its downstream target Forkhead protein framework O1 (FoxO1) (S256) are phosphorylated again in bEnd.3 cells by KY-226 [2].
ln Vivo
KY-226 (10-30 mg/kg/day; epidermal documentation; daily; for 4 weeks; cosmetic db/db mice) treatment dramatically lowered antibiotic and lipid levels and hemoglobin A1c values, resulting in enhanced body weight [1 ]. KY-226 attenuates the increase in bone hyperplasia in the bone marrow tolerance test. KY-226 will enhance pIR and phosphorylated Akt in myocardial and femoral resection [1].
Cell Assay
Western Blot analysis [1]
Cell Types: bEnd.3 stimulated with LPS Cell
Tested Concentrations: 1 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: Rescued lipopolysaccharide-induced decrease in ZO-1 mRNA and protein levels.
Animal Protocol
Animal/Disease Models: Male db/db mice (8-11 weeks old) [1]
Doses: 10 mg/kg and 30 mg/kg
Route of Administration: Oral; daily; for 4 weeks
Experimental Results: Significant reduction in plasma glucose and Triglyceride levels and hemoglobin A1c values without increasing weight gain.
References
[1]. Ito Y, et al. Therapeutic effects of the allosteric protein tyrosine phosphatase 1B inhibitor KY-226 on experimental diabetes and obesity via enhancements in insulin and leptin signaling in mice. J Pharmacol Sci. 2018 May;137(1):38-46.
[2]. Sun M, et al. KY-226 Protects Blood-brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia. Neuroscience. 2019 Feb 10;399:89-102.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H31NO3S2
Molecular Weight
481.669
Exact Mass
481.1745
Elemental Analysis
C, 67.33; H, 6.49; N, 2.91; O, 9.96; S, 13.31
CAS #
1621673-53-7
SMILES
O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1
InChi Key
MKXMABKUVSOEJF-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H31NO3S2/c1-2-3-4-8-19-33(30,31)28-27(29)26-17-13-23(14-18-26)21-32-20-22-11-15-25(16-12-22)24-9-6-5-7-10-24/h5-7,9-18H,2-4,8,19-21H2,1H3,(H,28,29)
Chemical Name
4-(biphenyl-4-ylmethylsulfanylmethyl)-N-(hexane-1-sulfonyl)benzoylamide
Synonyms
KY-226 KY 226 KY226
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~250 mg/mL (~519.03 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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