H-7

BML-EI148

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PKC inhibitor

Inhibits PKA (K_i=3.0μM), PKG (K_i=5.8μM), MLCK (K_i=97μM) and PKC (K_i=6μM). Also inhibits myosin light chain kinase. Induces apoptotic DNA fragmentation and cell death. Inhibits telomerase activity in treated NPC-076 cells. Cell permeable.

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Product Details

Alternative Name	(±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
Appearance	White to light yellow solid.
CAS	108930-17-2
Couple Target	MLCK, PKA, PKC, PKG, Telomerase
Couple Type	Inhibitor
Formula	C₁₄H₁₇N₃O₂S . 2 HCl
MW	364.3
Purity	≥98% (TLC)
Solubility	Soluble in water (50mg/ml), 100% ethanol or DMSO.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store, as supplied, at 0-4°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Handling	Protect from light.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; Biochem. Biophys. Res. Commun. 241, 730 (1997), Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996), Abstract — Full Text
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994), Abstract
Modulation of neutrophil superoxide generation by inhibitors of protein kinase C, calmodulin, diacylglycerol and myosin light chain kinases, and peptidyl prolyl cis-trans isomerase: H. Bergstrand, et al.; J. Pharmacol. Exp. Ther. 263, 1334 (1992), Abstract
Cellular interactions with the extracellular matrix are coupled to diverse transmembrane signaling pathways.: C. Gimond and M. Aumailley; Exp. Cell Res. 203, 365 (1992), Abstract
The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source: J. Quick, et al.; BBRC 187, 657 (1992), Abstract
Blockade of the spinal excitatory effect of cAMP on the startle reflex by intrathecal administration of the isoquinoline sulfonamide H-8: comparison to the protein kinase C inhibitor H-7: N.M. Boulis & M. Davis; Brain Res. 525, 198 (1990), Abstract
Potent selective inhibition of 7-O-methyl UCN-01 against protein kinase C: I. Takahashi, et al.; J. Pharmacol. Exp. Ther. 255, 1218 (1990), Abstract
Stimulus-dependent inhibition of platelet aggregation by the protein kinase C inhibitors polymyxin B, H-7 and staurosporine: C. Schächtele, et al.; BBRC 151, 542 (1988), Abstract
1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets: S. Kawamoto & H. Hidaka; BBRC 125, 258 (1984), Abstract

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H-7

BML-EI148

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