Delcasertib is a potent and selective inhibitor of δ-protein kinase C (δPKC).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 321 | |
2 mg | In stock | $ 545 | |
4 mg | In stock | $ 865 | |
10 mg | In stock | $ 1879 | |
20 mg | In stock | $ 3006 |
Description | Delcasertib 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 | BMS-875944, KAI-9803 |
CAS No. | 949100-39-4 |
Chemical Formula | C120H199N45O34S2 |
Molecular Weight | 2880.31 |
Solubility | DMSO: 99 mg/mL(34.37 mM) |
Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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