PY-60
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MedKoo CAT#: 465543

CAS#: 2765218-56-0

Description: PY-60 is a novel activator of YAP, promoting expansion of epidermal keratinocytes ex vivo and in vivo, targeting ANXA2 to activate YAP, activating a robust, YAP- dependent transcriptional program in multiple cell types. Chemical proteomics revealed the relevant target of PY-60 to be annexin A2 (ANXA2), a protein that directly associates with YAP at the cell membrane in response to increased cell density. PY-60 treatment liberates ANXA2 from the membrane, ultimately promoting a phosphatase-bound, nonphosphorylated and transcriptionally active form of YAP.


Chemical Structure

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PY-60
CAS# 2765218-56-0

Theoretical Analysis

MedKoo Cat#: 465543
Name: PY-60
CAS#: 2765218-56-0
Chemical Formula: C16H15N3O2S
Exact Mass: 313.09
Molecular Weight: 313.380
Elemental Analysis: C, 61.32; H, 4.82; N, 13.41; O, 10.21; S, 10.23

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to Ship
10mg USD 250 Ready to Ship
25mg USD 450 Ready to Ship
50mg USD 750 Ready to Ship
100mg USD 1350 Ready to Ship
200mg USD 2350 Ready to Ship
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Synonym: PY-60; PY 60; PY60;

IUPAC/Chemical Name: 5-phenyl-N-(3-(thiazol-2-yl)propyl)isoxazole-3-carboxamide

InChi Key: UFASECSYKSMYET-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H15N3O2S/c20-16(18-8-4-7-15-17-9-10-22-15)13-11-14(21-19-13)12-5-2-1-3-6-12/h1-3,5-6,9-11H,4,7-8H2,(H,18,20)

SMILES Code: O=C(C1=NOC(C2=CC=CC=C2)=C1)NCCCC3=NC=CS3

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: PY-60 is a specific activator of YAP transcriptional activity that targets annexin ANXA2 (Kd = 1.4 µM). PY-60 directly binds to ANXA2 and antagonizes its repression of YAP activity.
In vitro activity: This study reports of PY-60, which robustly activated YAP transcriptional activity in vitro. Chemical proteomics revealed the relevant target of PY-60 to be ANXA2. PY-60 treatment frees ANXA2 from the cell membrane, promoting a phosphatase-bound, nonphosphorylated and transcriptionally active form of YAP. Reference: Nat Chem Biol. 2021 Jul;17(7):767-775. https://pubmed.ncbi.nlm.nih.gov/33723431/
In vivo activity: Topical application of PY-60 promoted regenerative repair of cutaneous wounds in pig and human models. Reference: Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. https://pubmed.ncbi.nlm.nih.gov/37399395/

Preparing Stock Solutions

The following data is based on the product molecular weight 313.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Chen J, Su X, Tan Q, Pu H, Zhang L, Kang Y, Tang Y, Zhao X, Hou W, Qian S, Deng S, Hou L, Gao Y. Effect of cell density on the malignant biological behavior of breast cancer by altering the subcellular localization of ANXA2 and its clinical implications. Clin Transl Oncol. 2022 Nov;24(11):2136-2145. doi: 10.1007/s12094-022-02865-0. Epub 2022 Jul 1. PMID: 35778647. 2. Shalhout SZ, Yang PY, Grzelak EM, Nutsch K, Shao S, Zambaldo C, Iaconelli J, Ibrahim L, Stanton C, Chadwick SR, Chen E, DeRan M, Li S, Hull M, Wu X, Chatterjee AK, Shen W, Camargo FD, Schultz PG, Bollong MJ. YAP-dependent proliferation by a small molecule targeting annexin A2. Nat Chem Biol. 2021 Jul;17(7):767-775. doi: 10.1038/s41589-021-00755-0. Epub 2021 Mar 15. PMID: 33723431. 3. Grzelak EM, Elshan NGRD, Shao S, Bulos ML, Joseph SB, Chatterjee AK, Chen JJ, Nguyên-Trân V, Schultz PG, Bollong MJ. Pharmacological YAP activation promotes regenerative repair of cutaneous wounds. Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. doi: 10.1073/pnas.2305085120. Epub 2023 Jul 3. PMID: 37399395; PMCID: PMC10334740.
In vitro protocol: 1. Chen J, Su X, Tan Q, Pu H, Zhang L, Kang Y, Tang Y, Zhao X, Hou W, Qian S, Deng S, Hou L, Gao Y. Effect of cell density on the malignant biological behavior of breast cancer by altering the subcellular localization of ANXA2 and its clinical implications. Clin Transl Oncol. 2022 Nov;24(11):2136-2145. doi: 10.1007/s12094-022-02865-0. Epub 2022 Jul 1. PMID: 35778647. 2. Shalhout SZ, Yang PY, Grzelak EM, Nutsch K, Shao S, Zambaldo C, Iaconelli J, Ibrahim L, Stanton C, Chadwick SR, Chen E, DeRan M, Li S, Hull M, Wu X, Chatterjee AK, Shen W, Camargo FD, Schultz PG, Bollong MJ. YAP-dependent proliferation by a small molecule targeting annexin A2. Nat Chem Biol. 2021 Jul;17(7):767-775. doi: 10.1038/s41589-021-00755-0. Epub 2021 Mar 15. PMID: 33723431.
In vivo protocol: 1. Grzelak EM, Elshan NGRD, Shao S, Bulos ML, Joseph SB, Chatterjee AK, Chen JJ, Nguyên-Trân V, Schultz PG, Bollong MJ. Pharmacological YAP activation promotes regenerative repair of cutaneous wounds. Proc Natl Acad Sci U S A. 2023 Jul 11;120(28):e2305085120. doi: 10.1073/pnas.2305085120. Epub 2023 Jul 3. PMID: 37399395; PMCID: PMC10334740.

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1: Shalhout SZ, Yang PY, Grzelak EM, Nutsch K, Shao S, Zambaldo C, Iaconelli J, Ibrahim L, Stanton C, Chadwick SR, Chen E, DeRan M, Li S, Hull M, Wu X, Chatterjee AK, Shen W, Camargo FD, Schultz PG, Bollong MJ. YAP-dependent proliferation by a small molecule targeting annexin A2. Nat Chem Biol. 2021 Jul;17(7):767-775. doi: 10.1038/s41589-021-00755-0. Epub 2021 Mar 15. PMID: 33723431.