130964-39-5 Usage
Description
H-89 DIHYDROCHLORIDE HYDRATE is a white solid that functions as a selective inhibitor of Protein Kinase A (cyclic AMP-dependent Protein Kinase) with an inhibitory constant of 0.0048 uM. It has been widely utilized in various biological and medical applications due to its ability to inhibit specific protein kinases.
Uses
Used in Biological Research:
H-89 DIHYDROCHLORIDE HYDRATE is used as a research tool for inhibiting protein kinase A in different cell types, such as Leydig cells, primary calvarial osteoblasts (pOBs), rat granulosa cell line (LH-15 cells), and human umbilical vein endothelial cells (HUVECs). This application aids scientists in studying the role of protein kinase A in cellular processes and its potential involvement in various diseases.
Used in Pharmaceutical Development:
H-89 DIHYDROCHLORIDE HYDRATE is used as a lead compound in the development of drugs targeting protein kinase A-related pathways. By inhibiting this enzyme, it may help in the treatment of conditions where protein kinase A plays a significant role, such as certain types of cancer or inflammatory diseases.
Used in Drug Screening:
H-89 DIHYDROCHLORIDE HYDRATE is used as a reference compound in drug screening assays to identify new molecules with similar inhibitory properties. This helps in the discovery of novel therapeutic agents that can modulate protein kinase A activity and potentially treat related disorders.
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].
Check Digit Verification of cas no
The CAS Registry Mumber 130964-39-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,0,9,6 and 4 respectively; the second part has 2 digits, 3 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 130964-39:
(8*1)+(7*3)+(6*0)+(5*9)+(4*6)+(3*4)+(2*3)+(1*9)=125
125 % 10 = 5
So 130964-39-5 is a valid CAS Registry Number.
