Product Name :
PTP Inhibitor IV
Description:
IC50: 1.8, 2.5, 8.4, 13, 20, 6.4, and 6.7 μM for SHP-2, PTP1B, PTP-ε, PTP-Meg-2, PTP-σ, PTP-β, and PTP-μ, respectively PTP Inhibitor IV is a protein tyrosine phosphatases (PTPs) inhibitor. PTPs are reported to be important in the regulation of various signal transduction processes. Enzymes of this class are considered as potential therapeutic targets in the treatment of various diseases including inflammation, diabetes, as well as cancer. However, previously identified PTP inhibitors are peptide-based containing a highly charged component, which usually lack membrane permeability resulting in their limited utility in the inhibition of intracellular phosphatases. In vitro: PTP inhibitor IV was identified as an uncharged, 1,4-di-substituted, phenyl-linked bis-trifluoromethylsulfonamido phosphate mimetic acting as a competitive, reversible, and active-site directed inhibitor. It was noticed that PTP inhibitor IV showed greatly increased potency not only on PTP1B but also on the phosphatases SHP-2 and Mu.{{Alpidem} MedChemExpress|{Alpidem} Neuronal Signaling|{Alpidem} Biological Activity|{Alpidem} Data Sheet|{Alpidem} supplier|{Alpidem} Cancer} Moreover, the interaction of the second SO2CF3 moiety in PTP inhibitor IV with conserved Arg residue of PTP might explain the increased inhibitory potency towards other PTPs in addition to PTP1B . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.
CAS:
329317-98-8
Molecular Weight:
608.62
Formula:
C26H26F6N2O4S2
Chemical Name:
1,1,1-trifluoro-N-{4-[2-(4-{2-[4-(trifluoromethanesulfonamido)phenyl]propan-2-yl}phenyl)propan-2-yl]phenyl}methanesulfonamide
Smiles :
CC(C)(C1C=CC(=CC=1)C(C)(C)C1C=CC(=CC=1)NS(=O)(=O)C(F)(F)F)C1C=CC(=CC=1)NS(=O)(=O)C(F)(F)F
InChiKey:
JWNAVYMNAQDLHX-UHFFFAOYSA-N
InChi :
InChI=1S/C26H26F6N2O4S2/c1-23(2,19-9-13-21(14-10-19)33-39(35,36)25(27,28)29)17-5-7-18(8-6-17)24(3,4)20-11-15-22(16-12-20)34-40(37,38)26(30,31)32/h5-16,33-34H,1-4H3
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Bexmarilimab} MedChemExpress|{Bexmarilimab} Purity & Documentation|{Bexmarilimab} Description|{Bexmarilimab} manufacturer|{Bexmarilimab} Cancer}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
IC50: 1.8, 2.5, 8.4, 13, 20, 6.4, and 6.7 μM for SHP-2, PTP1B, PTP-ε, PTP-Meg-2, PTP-σ, PTP-β, and PTP-μ, respectively PTP Inhibitor IV is a protein tyrosine phosphatases (PTPs) inhibitor. PTPs are reported to be important in the regulation of various signal transduction processes.PMID:36014399 Enzymes of this class are considered as potential therapeutic targets in the treatment of various diseases including inflammation, diabetes, as well as cancer. However, previously identified PTP inhibitors are peptide-based containing a highly charged component, which usually lack membrane permeability resulting in their limited utility in the inhibition of intracellular phosphatases. In vitro: PTP inhibitor IV was identified as an uncharged, 1,4-di-substituted, phenyl-linked bis-trifluoromethylsulfonamido phosphate mimetic acting as a competitive, reversible, and active-site directed inhibitor. It was noticed that PTP inhibitor IV showed greatly increased potency not only on PTP1B but also on the phosphatases SHP-2 and Mu. Moreover, the interaction of the second SO2CF3 moiety in PTP inhibitor IV with conserved Arg residue of PTP might explain the increased inhibitory potency towards other PTPs in addition to PTP1B . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.|Product information|CAS Number: 329317-98-8|Molecular Weight: 608.62|Formula: C26H26F6N2O4S2|Chemical Name: 1,1,1-trifluoro-N-{4-[2-(4-{2-[4-(trifluoromethanesulfonamido)phenyl]propan-2-yl}phenyl)propan-2-yl]phenyl}methanesulfonamide|Smiles: CC(C)(C1C=CC(=CC=1)C(C)(C)C1C=CC(=CC=1)NS(=O)(=O)C(F)(F)F)C1C=CC(=CC=1)NS(=O)(=O)C(F)(F)F|InChiKey: JWNAVYMNAQDLHX-UHFFFAOYSA-N|InChi: InChI=1S/C26H26F6N2O4S2/c1-23(2,19-9-13-21(14-10-19)33-39(35,36)25(27,28)29)17-5-7-18(8-6-17)24(3,4)20-11-15-22(16-12-20)34-40(37,38)26(30,31)32/h5-16,33-34H,1-4H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|