PS432
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MedKoo CAT#: 561835

CAS#: 2083630-26-4

Description: PS432 is an allosteric inhibitor of atypical PKCs. It has been shown to target the PIF-pocket and significantly reduce tumor growth without side effects in mouse xenograft model.

Chemical Structure

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PS432
CAS# 2083630-26-4
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 561835
Name: PS432
CAS#: 2083630-26-4
Chemical Formula: C25H19ClN2O5S
Exact Mass: 494.07
Molecular Weight: 494.940
Elemental Analysis: C, 60.67; H, 3.87; Cl, 7.16; N, 5.66; O, 16.16; S, 6.48

Price and Availability

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5mg USD 230
25mg USD 570
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Synonym: PS432; PS-432; PS 432;

IUPAC/Chemical Name: 2-[5-(4-Chloro-phenyl)-furan-2-yl]-4-hydroxy-1-(6-methyl-benzothiazol-2-yl)-5-oxo-2,5-dihydro-1H-pyrrole-3-carboxylic acid ethyl ester

InChi Key: NBZPOMWJBSLLCT-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H19ClN2O5S/c1-3-32-24(31)20-21(18-11-10-17(33-18)14-5-7-15(26)8-6-14)28(23(30)22(20)29)25-27-16-9-4-13(2)12-19(16)34-25/h4-12,21,29H,3H2,1-2H3

SMILES Code: O=C(C1=C(O)C(N(C2=NC3=CC=C(C)C=C3S2)C1C4=CC=C(C5=CC=C(Cl)C=C5)O4)=O)OCC

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: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: PS432 is a PKC inhibitor with IC50s of 16.9 μM (PKCι) and 18.5 μM (PKCζ), respectively.
In vitro activity: In this study, researchers utilized 2D difference gel electrophoresis to identify three isoforms of K8 significantly increased in colon tumors compared to normal tissue. There were elevated levels of PS24, PS432, and PS74 in tumors. Blocking EGFR signaling led to a substantial reduction in PS74 and PS432 levels, resulting in increased apoptosis in Caco2 cells. Reference: ISRN Mol Biol. 2012 Jan 31;2012:706545. https://pubmed.ncbi.nlm.nih.gov/27398237/
In vivo activity: To be determined

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.0 202.04

Preparing Stock Solutions

The following data is based on the product molecular weight 494.94 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. Arencibia JM, Fröhner W, Krupa M, Pastor-Flores D, Merker P, Oellerich T, Neimanis S, Schmithals C, Köberle V, Süß E, Zeuzem S, Stark H, Piiper A, Odadzic D, Schulze JO, Biondi RM. An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms. ACS Chem Biol. 2017 Feb 17;12(2):564-573. doi: 10.1021/acschembio.6b00827. Epub 2017 Jan 13. PMID: 28045490. 2. Arentz G, Chataway T, Condina MR, Price TJ, Hoffmann P, Hardingham JE. Increased Phospho-Keratin 8 Isoforms in Colorectal Tumors Associated with EGFR Pathway Activation and Reduced Apoptosis. ISRN Mol Biol. 2012 Jan 31;2012:706545. doi: 10.5402/2012/706545. PMID: 27398237; PMCID: PMC4908239.
In vitro protocol: 1. Arencibia JM, Fröhner W, Krupa M, Pastor-Flores D, Merker P, Oellerich T, Neimanis S, Schmithals C, Köberle V, Süß E, Zeuzem S, Stark H, Piiper A, Odadzic D, Schulze JO, Biondi RM. An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms. ACS Chem Biol. 2017 Feb 17;12(2):564-573. doi: 10.1021/acschembio.6b00827. Epub 2017 Jan 13. PMID: 28045490. 2. Arentz G, Chataway T, Condina MR, Price TJ, Hoffmann P, Hardingham JE. Increased Phospho-Keratin 8 Isoforms in Colorectal Tumors Associated with EGFR Pathway Activation and Reduced Apoptosis. ISRN Mol Biol. 2012 Jan 31;2012:706545. doi: 10.5402/2012/706545. PMID: 27398237; PMCID: PMC4908239.
In vivo protocol: To be determined

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1: Arencibia JM, Fröhner W, Krupa M, Pastor-Flores D, Merker P, Oellerich T, Neimanis S, Schmithals C, Köberle V, Süß E, Zeuzem S, Stark H, Piiper A, Odadzic D, Schulze JO, Biondi RM. An Allosteric Inhibitor Scaffold Targeting the PIF-Pocket of Atypical Protein Kinase C Isoforms. ACS Chem Biol. 2017 Feb 17;12(2):564-573. doi: 10.1021/acschembio.6b00827. Epub 2017 Jan 13. PubMed PMID: 28045490.

2: Arentz G, Chataway T, Condina MR, Price TJ, Hoffmann P, Hardingham JE. Increased Phospho-Keratin 8 Isoforms in Colorectal Tumors Associated with EGFR Pathway Activation and Reduced Apoptosis. ISRN Mol Biol. 2012 Jan 31;2012:706545. doi: 10.5402/2012/706545. eCollection 2012. PubMed PMID: 27398237; PubMed Central PMCID: PMC4908239.