INH1 - CAS 313553-47-8
Catalog number:
313553-47-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H16N2OS
Molecular Weight:
308.40
COA:
Inquire
Targets:
Others
Description:
INH1 is a cell-permeable Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction.
Publictions citing BOC Sciences Products
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Purity:
>98%
Synonyms:
IBT 13131
MSDS:
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1.A Synthetic Factor XIIa Inhibitor Blocks Selectively Intrinsic Coagulation Initiation.
Baeriswyl V1, Calzavarini S2,3, Chen S1, Zorzi A1, Bologna L2,3, Angelillo-Scherrer A2,3, Heinis C1. ACS Chem Biol. 2015 Aug 21;10(8):1861-70. doi: 10.1021/acschembio.5b00103. Epub 2015 May 19.
Coagulation factor XII (FXII) inhibitors are of interest for the study of the protease in the intrinsic coagulation pathway, for the suppression of contact activation in blood coagulation assays, and they have potential application in antithrombotic therapy. However, synthetic FXII inhibitors developed to date have weak binding affinity and/or poor selectivity. Herein, we developed a peptide macrocycle that inhibits activated FXII (FXIIa) with an inhibitory constant Ki of 22 nM and a selectivity of >2000-fold over other proteases. Sequence and structure analysis revealed that one of the two macrocyclic rings of the in vitro evolved peptide mimics the combining loop of corn trypsin inhibitor, a natural protein-based inhibitor of FXIIa. The synthetic inhibitor blocked intrinsic coagulation initiation without affecting extrinsic coagulation. Furthermore, the peptide macrocycle efficiently suppressed plasma coagulation triggered by contact of blood with sample tubes and allowed specific investigation of tissue factor initiated coagulation.
2.The Coagulation Factor XIIa Inhibitor rHA-Infestin-4 Improves Outcome after Cerebral Ischemia/Reperfusion Injury in Rats.
Krupka J1, May F1, Weimer T1, Pragst I1, Kleinschnitz C2, Stoll G2, Panousis C3, Dickneite G1, Nolte MW1. PLoS One. 2016 Jan 27;11(1):e0146783. doi: 10.1371/journal.pone.0146783. eCollection 2016.
BACKGROUND AND PURPOSE: Ischemic stroke provokes severe brain damage and remains a predominant disease in industrialized countries. The coagulation factor XII (FXII)-driven contact activation system plays a central, but not yet fully defined pathogenic role in stroke development. Here, we investigated the efficacy of the FXIIa inhibitor rHA-Infestin-4 in a rat model of ischemic stroke using both a prophylactic and a therapeutic approach.
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CAS 313553-47-8 INH1

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