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Delcasertib

Catalog No. T11740   CAS 949100-39-4
Synonyms: KAI-9803, BMS-875944

Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).

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Delcasertib Chemical Structure
Delcasertib, CAS 949100-39-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 213.00
5 mg In stock $ 538.00
10 mg In stock $ 778.00
25 mg In stock $ 1,180.00
50 mg In stock $ 1,620.00
100 mg In stock $ 2,180.00
1 mL * 10 mM (in DMSO) In stock $ 1,780.00
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Purity: 99.96%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).
In vitro Delcasertib is composed of a selective δ-protein kinase C (δPKC) inhibitor peptide derived from the δV1-1 portion of δPKC (termed 'cargo peptide”), conjugated reversibly to the cell-penetrating peptide 11-amino acid, arginine-rich sequence of the HIV type 1 transactivator protein (TAT47–57; termed 'carrier peptide”) via a disulfide bond.
In vivo KAI-9803 ameliorates pathological conditions in acute myocardial infarction and reduce pain via specific modulation of membrane-translocation of PKC delta or epsilon. Delcasertib has an acceptable safety and tolerability profile when delivered via intracoronary injection during primary percutaneous coronary intervention for ST-segment elevation myocardial infarction.Delcasertib administration at the end of ischemia has been found to reduce cardiac damage caused by ischemia-reperfusion in a rat model of acute myocardial infarction. 14C-KAI-9803 is rapidly delivered to many tissues, including the heart (1.21 μg eq/g tissue), while being quickly cleared from the systemic circulation. The distribution of Delcasertib to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47–57.
Synonyms KAI-9803, BMS-875944
Molecular Weight 2880.28
Formula C120H199N45O34S2
CAS No. 949100-39-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 99 mg/mL(34.37 mM)

TargetMolReferences and Literature

1. Miyaji Y, et al. Distribution of KAI-9803, a novel δ-protein kinase C inhibitor, after intravenous administration to rats. Drug Metab Dispos. 2011 Oct;39(10):1946-53. 2. Bates E, et al. Intracoronary KAI-9803 as an adjunct to primary percutaneous coronary intervention for acute ST-segment elevation myocardial infarction. Circulation. 2008 Feb 19;117(7):886-96.

Related compound libraries

This product is contained In the following compound libraries:
Peptide Compound Library Reprogramming Compound Library Inhibitor Library ReFRAME Related Library Bioactive Compounds Library Max NO PAINS Compound Library Bioactive Compound Library

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Keywords

Delcasertib 949100-39-4 Chromatin/Epigenetic Cytoskeletal Signaling PKC BMS 875944 Inhibitor KAI-9803 KAI 9803 inhibit KAI9803 Protein kinase C BMS-875944 BMS875944 inhibitor

 

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