ChemicalBook Product Catalog Biochemical Engineering Inhibitors KY-226

KY-226

Product NameKY-226
CAS1621673-53-7
MFC27H31NO3S2
MW481.67
EINECS
MOL File1621673-53-7.mol

Chemical Properties

Density	1.186±0.06 g/cm3(Predicted)
storage temp.	-20°
solubility	Soluble in DMSO (>25 mg/ml).
form	solid
pka	3.91±0.40(Predicted)
color	Off-white
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
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)
InChIKey	MKXMABKUVSOEJF-UHFFFAOYSA-N
SMILES	O=C(NS(=O)(CCCCCC)=O)C1=CC=C(CSCC2=CC=C(C3=CC=CC=C3)C=C2)C=C1

Safety Information

WGK Germany	WGK 3
Storage Class	11 - Combustible Solids

Usage And Synthesis

Description

KY-226 (CAS 1621673-53-7) is a selective allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor (IC50= 250 nM) with no activity at PPARγ.1It significantly reduced plasma glucose, triglyceride, and A1c levels without weight gain in db/db mice.2It has been suggested that KY-226’s anti-diabetic effects occurviaenhancements in insulin signaling and anti-obesity effects via leptin signaling enhancements.2KY-226 has also been shown to protect neurons from cerebral ischemia.3This effect is mediated by restoration of tight junction proteinsviaactivation of the Akt/FoxO1 pathway.4

Uses

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].

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.

References

[1] KO MORISHITA. Novel Non-carboxylate Benzoylsulfonamide-Based Protein Tyrosine Phosphatase 1B Inhibitors with Non-competitive Actions.[J]. Chemical & pharmaceutical bulletin, 2017, 65 12: 1144-1160. DOI:10.1248/cpb.c17-00635
[2] YUMA ITO . 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]. Journal of pharmacological sciences, 2018, 137 1: Pages 38-46. DOI:10.1016/j.jphs.2018.03.001
[3] MEILING SUN. Neuroprotective effects of protein tyrosine phosphatase 1B inhibitor on cerebral ischemia/reperfusion in mice[J]. Brain Research, 2018, 1694: Pages 1-12. DOI:10.1016/j.brainres.2018.04.029
[4] MEILING SUN Kohji F Yasuharu Shinoda. KY-226 Protects Blood–brain Barrier Function Through the Akt/FoxO1 Signaling Pathway in Brain Ischemia[J]. Neuroscience, 2019, 399: Pages 89-102. DOI:10.1016/j.neuroscience.2018.12.024

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