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PY-60

Catalog No.GC62424

PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 ?M.

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PY-60 Chemical Structure

Cas No.: 2765218-56-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$347.00
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5 mg
$315.00
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10 mg
$522.00
In stock
25 mg
$990.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity[1].

PY-60 targets ANXA2 to activate YAP[1].PY-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 (EC50= 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)[1]. PY-60 activates a proproliferative, YAP-dependent transcriptional program in the adult animal capable of remodeling the epidermis through proliferation[1]. PY-60 liberates the ANXA2-YAP complex from the cell membrane and competes for ANXA2 binding of phosphoinositides[1].

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[1].

[1]. Shalhout SZ, et al. YAP-dependent proliferation by a small molecule targeting annexin A2. Nat Chem Biol. 2021;17(7):767-775.

Chemical Properties

Cas No. 2765218-56-0 SDF
Formula C16H15N3O2S M.Wt 313.37
Solubility DMSO : 100 mg/mL (319.11 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.1911 mL 15.9556 mL 31.9112 mL
5 mM 0.6382 mL 3.1911 mL 6.3822 mL
10 mM 0.3191 mL 1.5956 mL 3.1911 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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