|
| | H-89 DIHYDROCHLORIDE HYDRATE Basic information |
| Product Name: | H-89 DIHYDROCHLORIDE HYDRATE | | Synonyms: | H-89 DIHYDROCHLORIDE HYDRATE;H-89 hydrate dihydrochloride;H-89 dihydrochloride hydrate,N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide dihydrochloride;5-IsoquinolinesulfonaMide, N-[2-[[3-(4-broMophenyl)-2-propenyl]aMino]ethyl]-, dihydrochloride;N-[2-[[3-(4-BroMophenyl)-2-propen-1-yl]aMino]ethyl]-5-isoquinolinesulfonaMide Hydrochloride;H 89 2HCl;Protein kinase inhibitor H-89 dihydrochloride;(E)-N-(2-(4-bromocinnamylamino)ethyl)isoquinoline-5-sulfonamide dihydrochloride | | CAS: | 130964-39-5 | | MF: | C20H20BrN3O2S.2ClH.H2O | | MW: | 537.304 | | EINECS: | | | Product Categories: | Inhibitors;Akt;Protein Kinase Inhibitors and Activators;PI3K/Akt/mTOR;mTOR;PI3K | | Mol File: | 130964-39-5.mol |  |
| | H-89 DIHYDROCHLORIDE HYDRATE Chemical Properties |
| Melting point | 195-200°C | | storage temp. | Inert atmosphere,2-8°C | | solubility | H2O: ≥10mg/mL | | form | powder | | color | off-white |
| Safety Statements | 22-24/25 | | WGK Germany | 3 | | HS Code | 2935909099 |
| | H-89 DIHYDROCHLORIDE HYDRATE Usage And Synthesis |
| Chemical Properties | White Solid | | Uses | H-89 dihydrochloride hydrate has been used in the inhibition of protein kinase A in Leydig cells, primary calvarial osteoblasts (pOBs), rat granulosa cell line (LH-15 cells) and human umbilical vein endothelial cells (HUVECs). | | Uses | Selective inhibitor of Protein Kinase A (cyclic AMP-dependeant Protein Kinase) with an inhibitory constant of
0.0048 uM. | | Definition | ChEBI: N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide dihydrochloride is a hydrochloride salt prepared from N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide and two equivalents of hydrogen chloride. It has a role as an EC 2.7.11.11 (cAMP-dependent protein kinase) inhibitor. It contains a N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide(2+). | | Biological Activity | h 89 2hcl is a potent pka inhibitor. in a cell-free assay, the ki of h 89 is 48 nm, 10-fold selective for pka than pkg and 500-fold greater selectivity than pkc, mlck, calmodulin kinase ii and casein kinase i/ii [1].[1]. chijiwa t, mishima a, hagiwara m, et al. inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic amp-dependent protein kinase, n-[2-(p-bromocinnamylamino) ethyl]-5-isoquinolinesulfonamide (h-89), of pc12d pheochromocytoma cells[j]. journal of biological chemistry, 1990, 265(9): 5267-5272.[2]. lochner a, moolman j a. the many faces of h89: a review[j]. cardiovascular drug reviews, 2006, 24(3‐4): 261-274.[3]. lee t h, linstedt a d. potential role for protein kinases in regulation of bidirectional endoplasmic reticulum-to-golgi transport revealed by protein kinase inhibitor h89[j]. molecular biology of the cell, 2000, 11(8): 2577-2590. | | Biochem/physiol Actions | H-89 dihydrochloride hydrate is a selective inhibitor of protein kinase A (PKA). It also inhibits potassium (K+) current in rat myocytes. It mediates Na+ transport by interacting with α subunits of epithelial Na+ channel (ENaC). | | in vitro | in pc12d cells, pretreatment with h-89 dose-dependently inhibited the forskolin-induced protein phosphorylation, with no influence in intracellular cyclic amp levels. in pc12d cells, h-89 significantly inhibited the forskolin-induced neurite outgrowth. in pc12d cells, pretreatment with h-89 (30 μm) strikingly inhibited camp-dependent histone iib phosphorylation activity in cell lysates while showed no effects on other protein phosphorylation activity such as cgmp-dependent histone iib phosphorylation activity [1]. h 89 was a potent and selective pka inhibitor with ki of 48 nm in a cell-free assay [2]. h89 also inhibited s6k1, msk1, pka, rockii, pkbα and mapkap-k1b kinases with ic50 of 80, 120, 135, 270, 2600 and 2800 nm, respectively [2]. in the hypotonic medium, 50 μm h89, a concentration commonly used to inhibit pka, prevented the redistribution response. in normal medium, h89 (50 μm) induced the redistribution of ergic 53 to the er by 20 min [3]. | | storage | -20°C |
| | H-89 DIHYDROCHLORIDE HYDRATE Preparation Products And Raw materials |
|
