Delcasertib hydrochloride
Based on 3 publication(s) in Google Scholar
Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
For research use only. We do not sell to patients.
- Purity: 98.31%
- Formula: C120H200ClN45O34S2
- Molecular Weight:2916.74
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Storage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications Citing Use of MedChemExpress (MCE) Delcasertib hydrochloride
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Biological Activity
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δPKC |
Delcasertib (KAI-9803) 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) via a disulfide bond[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Delcasertib (KAI-9803) 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[1].
Delcasertib (KAI-9803) has been studied for the prevention of reperfusion injury in patients undergoing angioplasty after acute myocardial infarction[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male Crl:CD(SD) rats[1]
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Dosage:1 mg/kg (Pharmacokinetic Analysis).
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Administration:Via the femoral vein.
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Result:The distribution to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47-57.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Solid
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Molecular Weight 2916.74
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Formula C120H200ClN45O34S2
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Color White to off-white
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Synonyms
KAI-9803 hydrochloride; BMS-875944 hydrochloride
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Sequence
Sequence 1:Cys-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg;Sequence 1':Cys-Ser-Phe-Asn-Ser-Tyr-Glu-Leu-Gly-Ser-Leu (Disulfide bridge:Cys1-Cys1')
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Sequence Shortening
Sequence 1:CYGRKKRRQRRR;Sequence 1':CSFNSYELGSL (Disulfide bridge:Cys1-Cys1')
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2021 Mar;591(7851):620-626. PMID: 33731924 -
Diabetes
Epoxygenase Cyp2c44 regulates hepatic lipid metabolism and insulin signaling by controlling FATP2 localization and activation of the DAG/PKCδ axis. [Abstract]2024 May 14:db230493. PMID: 38743615 -
J Leukoc Biol
2025 Apr 23;117(4):qiaf019. PMID: 39946245
Solvent & Solubility
H2O : 100 mg/mL (34.28 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (17.14 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.3428 mL | 1.7142 mL | 3.4285 mL | 8.5712 mL |
| 5 mM | 0.0686 mL | 0.3428 mL | 0.6857 mL | 1.7142 mL | |
| 10 mM | 0.0343 mL | 0.1714 mL | 0.3428 mL | 0.8571 mL | |
| 15 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5714 mL | |
| 20 mM | 0.0171 mL | 0.0857 mL | 0.1714 mL | 0.4286 mL | |
| 25 mM | 0.0137 mL | 0.0686 mL | 0.1371 mL | 0.3428 mL | |
| 30 mM | 0.0114 mL | 0.0571 mL | 0.1143 mL | 0.2857 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.