PY-60 - ≥98% , CAS No.2765218-56-0

CAS: 2765218-56-0 Cat. No.: P650543 분자식: C₁₆H₁₅N₃O₂S 분자량: 313.37 PubChem CID: 155387479

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a K d of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity.

In Vitro

PY-60 targets ANXA2 to activate YAP. ?\nPY-60, a thiazole-substituted derivative, dose-dependently induces luciferase activity in 293A-TEAD-LUC cells in the presence or absence of serum when cells were plated at high cell density (EC 50 =?1.5 and 1.6?μM, respectively). PY-60 treatment also dose-dependently promoted the association of YAP and TEAD proteins in cells and induced the nuclear localization of YAP in response to increased cell density. PY-60 robustly increases the levels of YAP-controlled transcripts (that is, ANRKD1 , CYR61 and CTGF ) in 293A cells and other human cell lines (that is, MCF10A, HEK293T, H69 and HaCaT), but did not augment the levels of YAP itself ( YAP1 ). ?\nPY-60 activates a proproliferative, YAP-dependent transcriptional program in the adult animal capable of remodeling the epidermis through proliferation. ?\nPY-60 liberates the ANXA2-YAP complex from the cell membrane and competes for ANXA2 binding of phosphoinositides. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PY-60 (10?uM; applied topically to the dorsal skin of wild-type adult C57BL/6 mice over the course of 10?days) promotes a dramatic expansion of keratinocytes and K14-positive precursors, as assessed by hematoxylin and eosin and anti-K14 histological staining at the study end. PY-60 results in an approximate doubling of epidermal thickness, a result derived from an increased number of keratinocytes per unit length of skin . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

Specifications

사양 및 순도

≥98%

생화학 및 생리적 메커니즘

PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a K d of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity.

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

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작업 유형

ACTIVATOR

순수함

≥98%

이름과 식별자

• 이성체 SMILES: C1=CC=C(C=C1)C2=CC(=NO2)C(=O)NCCCC3=NC=CS3
• PubChem CID: 155387479
• 분자량: 313.37

화학 및 물리적 특성

• 용해성: DMSO : 100 mg/mL (319.11 mM; Need ultrasonic)