Delcasertib (KAI-9803) HCl is a specific inhibitor of delta protein kinase C (delta PKC). Delcasertib (KAI-9803) HCl improves ischemia-reperfusion injury in animal models of acute myocardial infarction.

Physicochemical Properties

Molecular Formula	C120H200CLN45O34S2
Molecular Weight	2916.74
Related CAS #	Delcasertib;949100-39-4
Appearance	Typically exists as solid at room temperature
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	δPKC
ln Vitro	Delcasertib hydrochloride (KAI-9803) is made up of an 11-amino acid (arginine-rich) cell-penetrating peptide and a specific delta-protein kinase C (δPKC) inhibitory peptide that is generated from the deltaV1-1 part of deltaPKC. Reversibly bonded disulfide links make up the acidic HIV type 1 transactivator sequence [1].
ln Vivo	Mice's liver, kidney, lung, heart, and brain exhibit specific inhibition of PKC translocation when administered intraperitoneally with delcasertib hydrochloride (KAI-9803) [1]. When given after the conclusion of ischemia, KAI-9803) was shown to lessen ischemia-reperfusion-induced heart damage in a rat model of acute myocardial infarction [1]. Patients having angioplasty following an acute myocardial infarction have been examined for the prevention of reperfusion injury with delcasertib hydrochloride (KAI-9803) [2].
Animal Protocol	Animal/Disease Models: Sixweeks old male Crl:CD(SD) rats[1] Doses: 1 mg/kg (pharmacokinetic/PK Analysis). Route of Administration: Via the femoral vein. Experimental Results: The distribution to tissues such as the liver, kidney, and heart is facilitated by the reversible conjugation to TAT47-57.
References	[1]. 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]. 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.

Solubility Data

Solubility (In Vitro)	H2O :~100 mg/mL (~34.28 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 50 mg/mL (17.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.3428 mL	1.7142 mL	3.4285 mL
	5 mM	0.0686 mL	0.3428 mL	0.6857 mL
	10 mM	0.0343 mL	0.1714 mL	0.3428 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.