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Delcasertib (KAI-9803) is a potent and selective inhibitor of δ-protein kinase C (δPKC).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $213 | In Stock | |
5 mg | $538 | In Stock | |
10 mg | $778 | In Stock | |
25 mg | $1,180 | In Stock | |
50 mg | $1,620 | In Stock | |
100 mg | $2,180 | In Stock | |
1 mL x 10 mM (in DMSO) | $1,780 | In Stock |
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. |
Alias | KAI-9803, BMS-875944 |
Molecular Weight | 2880.28 |
Formula | C120H199N45O34S2 |
Cas No. | 949100-39-4 |
Smiles | [C@H](CC1=CC=C(O)C=C1)(C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@@H](CC(C)C)C(O)=O)=O)CO)=O)=O)CC(C)C)=O)CCC(O)=O)=O)NC([C@@H](NC([C@@H](NC([C@H](CC2=CC=CC=C2)NC([C@@H](NC([C@H](CSSC[C@@H](C(N[C@@H](CC3=CC=C(O)C=C3)C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CCCNC(=N)N)C(O)=O)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCC(N)=O)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCCCN)=O)CCCCN)=O)CCCNC(=N)N)=O)=O)=O)N)N)=O)CO)=O)=O)CC(N)=O)=O)CO)=O |
Relative Density. | 1.54 g/cm3 (Predicted) |
Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 99 mg/mL (34.37 mM) | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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