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
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
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
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
100.0 |
202.04 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
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.
| 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
1: Xiang J, Zhang N, Du A, Li J, Luo M, Wang Y, Liu M, Yang L, Li X, Wang L, Liu Q, Chen D, Wang T, Bian XW, Qin ZY, Su L, Wen L, Wang B. A Ubiquitin-Dependent Switch on MEF2D Senses Pro-Metastatic Niche Signals to Facilitate Intrahepatic Metastasis of Liver Cancer. Adv Sci (Weinh). 2023 Dec;10(35):e2305550. doi: 10.1002/advs.202305550. Epub 2023 Oct 12. PMID: 37828611; PMCID: PMC10724427.
2: 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.
3: 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.
