Epsilon-V1-2 (ε-V1-2) is a PKCε-derived peptide and a selective PKCε inhibitor. Epsilon-V1-2 inhibits the transport of PKCε but not α-, β- and δPKC.

Physicochemical Properties

Molecular Formula	C37H65N9O13
Molecular Weight	843.96
Exact Mass	843.47
CAS #	182683-50-7
PubChem CID	10147482
Appearance	White to off-white solid powder
Density	1.3±0.1 g/cm3
Boiling Point	1280.1±65.0 °C at 760 mmHg
Flash Point	728.0±34.3 °C
Vapour Pressure	0.0±0.6 mmHg at 25°C
Index of Refraction	1.552
LogP	-1.22
Hydrogen Bond Donor Count	12
Hydrogen Bond Acceptor Count	15
Rotatable Bond Count	26
Heavy Atom Count	59
Complexity	1480
Defined Atom Stereocenter Count	9
SMILES	C[C@H]([C@@H](C(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)N)O
InChi Key	KNTBAGOTDJPUJV-XMTFRXHISA-N
InChi Code	InChI=1S/C37H65N9O13/c1-18(2)16-24(32(53)41-23(10-7-8-14-38)36(57)46-15-9-11-26(46)34(55)45-29(21(6)48)37(58)59)42-33(54)25(17-47)43-35(56)28(19(3)4)44-30(51)20(5)40-31(52)22(39)12-13-27(49)50/h18-26,28-29,47-48H,7-17,38-39H2,1-6H3,(H,40,52)(H,41,53)(H,42,54)(H,43,56)(H,44,51)(H,45,55)(H,49,50)(H,58,59)/t20-,21+,22-,23-,24-,25-,26-,28-,29-/m0/s1
Chemical Name	(4S)-4-amino-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[(2S)-2-[[(1S,2R)-1-carboxy-2-hydroxypropyl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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, avoid exposure to moisture.
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	PKCε
ln Vitro	Epsilon-V1-2 (ε-V1-2), a peptide generated from PKCε that has its particular receptor for activated C kinase (RACK) sited therein, inhibits PKCε translocation and decreases the insulin response to glucose[1]. Cardiomyocytes treated with Epsilon-V1 -2 (ε-V1-2; 1 µM, 24 hours) show considerable inhibition of Oleic acid (OA)-induced connexin 43 (Cx43) Ser368 phosphorylation and prevention of OA-induced gap junction disassembly[2].
ln Vivo	In a mouse heterotopic transplantation paradigm, Epsilon-V1-2 (20 mg/kg/day; osmotic pumps; daily; for 4 weeks) therapy dramatically increases the beating score. Epsilon-V1-2 lessens parenchymal fibrosis and the infiltration of T lymphocytes and macrophages into cardiac grafts. The increase in pro-fibrotic cytokine TGF-β and monocyte recruitment chemokine MCP-1 levels is nearly completely eliminated by epsilon-V1-2 treatment[3].
Animal Protocol	Animal/Disease Models: C57BL/6J mice transplanted the hearts of FVB mice[3] Doses: 20 mg/kg/day Route of Administration: 0.1 mL osmotic pumps implanted subcutaneously (sc); daily; for 4 weeks Experimental Results: Dramatically improved the beating score throughout the treatment.
References	[1]. Translocation inhibitors define specificity of protein kinase C isoenzymes in pancreatic beta-cells. J Biol Chem. 1997 Jan 17;272(3):1417-20. [2]. Mechanism of oleic acid-induced gap junctional disassembly in rat cardiomyocytes. J Mol Cell Cardiol. 2004 Sep;37(3):755-66. [3]. Pharmacological inhibition of epsilon PKC suppresses chronic inflammation in murine cardiac transplantation model. J Mol Cell Cardiol. 2007 Oct;43(4):517-22.

Solubility Data

Solubility (In Vitro)	H2O : 50 mg/mL (59.24 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 100 mg/mL (118.49 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	1.1849 mL	5.9245 mL	11.8489 mL
	5 mM	0.2370 mL	1.1849 mL	2.3698 mL
	10 mM	0.1185 mL	0.5924 mL	1.1849 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.