1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. Delcasertib

Delcasertib (Synonyms: KAI-9803; BMS-875944)

Cat. No.: HY-106262 Purity: 95.38%
Handling Instructions

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

Delcasertib Chemical Structure

Delcasertib Chemical Structure

CAS No. : 949100-39-4

Size Price Stock Quantity
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 990 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1990 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 Get quote
100 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Delcasertib:

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Description

Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI)[1][2].

IC50 & Target

δPKC

 

In Vitro

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 (TAT47–57; termed “carrier peptide”) via a disulfide bond[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Delcasertib (KAI-9803, a single intraperitoneal injection) in mice results in the selective inhibition of PKC translocation in the liver, kidney, lung, heart, and brain[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Six-week-old male Crl:CD(SD) rats[1].
Dosage: 1 mg/kg (Pharmacokinetic Analysis).
Administration: Via the femoral vein.
Result: The distribution to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47-57.
Clinical Trial
Molecular Weight

2880.28

Formula

C₁₂₀H₁₉₉N₄₅O₃₄S₂

CAS No.

949100-39-4

Sequence Shortening

Sequence 1:CYGRKKRRQRRR;Sequence 1':CSFNSYELGSL (Disulfide bridge:Cys1-Cys1’)

SMILES

[Sequence 1:Cys-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg; Sequence 1':Ser-Phe-Asn-Ser-Tyr-Glu-Leu-Gly-Ser-Leu (Disulfide bridge:Cys1-Cys1')]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (34.72 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3472 mL 1.7359 mL 3.4719 mL
5 mM 0.0694 mL 0.3472 mL 0.6944 mL
10 mM 0.0347 mL 0.1736 mL 0.3472 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 7.69 mg/mL (2.67 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (0.87 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (0.87 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 95.38%

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Keywords:

DelcasertibKAI-9803 BMS-875944KAI9803KAI 9803BMS875944BMS 875944BMS-875944PKCProtein kinase CInhibitorinhibitorinhibit

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