PT 1

PT 1 is a selective activator of AMPK with EC50 value of 0.3 μM for AMPK α1β1γ1 . AMP-activated protein kinase (AMPK) is serine/threonine protein kinase that involved in cellular energy homeostasis and acts as an energy sensor. AMPK is a heterotrimer and increases ATP generation . PT 1 is a selective AMPK activator. PT1 activated human AMPK α1394, AMPK α2398 and AMPK(α1β1γ1) with EC50 values of 8, 12 and 0.3 μM, respectively. PT1 exhibited maximum activity against AMPK(α1β1γ1) at concentration up to 5 μM. PT1 exhibited high selectivity for AMPK α catalytic subunit. PT1 activated truncated AMPK α1 subunit proteins including 313-335 aa with EC50 values of 8 μM, which was autoinhibitory domain. In HeLa cells without LKB1, PT1 induced AMPK and ACC phosphorylation, which were independent of LKB1. In human hepatoma HepG2 cells, PT1 dose-dependently reduced triacylglycerol and cholesterol content and induced AMPK and ACC phosphorylation . In incubated mouse muscle, PT-1 increased γ1-containing AMPK activity and increased the AMPK-dependent phosphorylation of ULK1 on Ser555. However, in HEK293 cells expressing human γ1-, γ2- or γ3-AMPK, PT-1 activated them equally .

Product information

CAS Number: 331002-70-1

Molecular Weight: 497.91

Formula: C23H16ClN3O6S

Chemical Name: 2-chloro-5-{[(2Z,5Z)-5-{[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene}-4-hydroxy-2,5-dihydro-1,3-thiazol-2-ylidene]amino}benzoic acid

Smiles: CC1=CC(=C(C=C1C)C1=CC=C(/C=C2\S/C(=N\C3=CC(=C(Cl)C=C3)C(O)=O)/N=C\2O)O1)N(=O)=O

InChiKey: RTHRCOIONCZINZ-JMIUGGIZSA-N

InChi: InChI=1S/C23H16ClN3O6S/c1-11-7-16(18(27(31)32)8-12(11)2)19-6-4-14(33-19)10-20-21(28)26-23(34-20)25-13-3-5-17(24)15(9-13)22(29)30/h3-10H,1-2H3,(H,29,30)(H,25,26,28)/b20-10-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.