612847-09-3 Usage
Description
AKTI-1/2 is an allosteric Akt (PKB) inhibitor, a type of protein kinase B, which plays a crucial role in regulating cell survival, growth, and metabolism. It is a promising pharmaceutical candidate for cancer treatment due to its ability to target the Akt pathway, which is often dysregulated in various cancers.
Uses
Used in Cancer Treatment:
AKTI-1/2 is used as a synergistic combination therapy for the treatment of cancer. It targets the Akt pathway, which is often dysregulated in various cancers, leading to uncontrolled cell growth and survival. By inhibiting the Akt pathway, AKTI-1/2 can effectively suppress tumor growth and enhance the efficacy of other cancer treatments.
Used in Drug Development:
AKTI-1/2 is also used in the development of novel drug therapies for cancer. Its allosteric inhibition mechanism offers a unique approach to targeting the Akt pathway, which can potentially lead to the discovery of new and more effective cancer treatments. Researchers are actively investigating the potential of AKTI-1/2 and similar compounds to improve cancer therapy outcomes and overcome drug resistance.
Biological Activity
akt inhibitor viii is a cell-permeable, reversible and potent, selective inhibitor of akt1, akt2 and akt3 with ic50 values of 58 nm, 210 nm and 2.12 μm, respectively.akt inhibitor viii has shown to remarkably increase anti-proliferation induced by furanodiene in human breast cancer cell mcf-7. akt inhibitor viii could enhance the furanodiene- stimulated akt and p-akt expression decreases as well as increase furanodiene-induced parp cleavage in mcf-7 cells [1].akt inhibitor viii has been revealed to inhibit igf-1-induced akt phosphorylation in a concentration-dependent manner. akt inhibitor viii has also been demonstrated to reduce pras40 phosphorylation in pc12 cells [2].
Enzyme inhibitor
This dual Akt1/Akt2 inhibitor (FW = 551.64 g/mol; CAS 612847-09-3; Soluble to 20 mM in DMSO with gentle warming), also named 1,3- dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]- methyl]-4-piperidinyl]-2H-benzimidazol-2-one, targets Protein kinase B (PKB) isoforms Akt1 (IC50 = 50 nM) and Akt2 (IC50 = 210 nM), serine/threonine-specific protein kinases that play a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration. Akti-1/2 is selective for Akt1 and 2 over a panel of other tyrosine and serine/threonine kinases. It also sensitizes LnCaP cells to TRAIL (TNF-related apoptosis-inducing ligand) induced apoptosis. Complete inhibition is achieved in liver cells treated with 1-10 μM. Akti-1/2 also blocks insulin regulation of PEP carboxykinase and glucose 6-phosphatase expression.
references
[1] zhong z1, dang y, yuan x, guo w, li y, tan w, cui j, lu j, zhang q, chen x, wang y. furanodiene, a natural product, inhibits breast cancer growth both in vitro and in vivo. cell physiol biochem. 2012;30(3):778-90.[2] wang h1, zhang q, zhang l, little pj, xie x, meng q, ren y, zhou l, gao g, quirion r, zheng w. insulin-like growth factor-1 induces the phosphorylation of pras40 via the pi3k/akt signaling pathway in pc12 cells. neurosci lett. 2012 may 10;516(1):105-9.
Check Digit Verification of cas no
The CAS Registry Mumber 612847-09-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,1,2,8,4 and 7 respectively; the second part has 2 digits, 0 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 612847-09:
(8*6)+(7*1)+(6*2)+(5*8)+(4*4)+(3*7)+(2*0)+(1*9)=153
153 % 10 = 3
So 612847-09-3 is a valid CAS Registry Number.
InChI:InChI=1/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)
