Apcin - CAS 300815-04-7
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C13H14Cl3N7O4
Molecular Weight:
438.65
COA:
Inquire
Targets:
APC
Description:
Apcin is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C), which is a large multimeric complex. It functions as a ubiquitin ligase, initiating the metaphase-anaphase transition and regulating ordered transitions through the cell cycle by controlling the ubiquitin-mediated proteolysis of cell cycle proteins. It competitively binds to the D-box binding site of Cdc20 and prevents substrate recognition and ubiquitylation required for continuation of mitosis. It synergistically increases apoptosis in multiple myeloma cells in combination with proTAME (prodrug of TAME). It also prolongs mitotic duration in RPE1 cells in combination with proTAME in vitro. It blocks mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe.
Purity:
≥98% by HPLC
Synonyms:
3-(2-Methyl-5-nitro-imidazol-1-yl)-N-(2,2,2-trichloro-1-phenylamino-ethyl)-propionamide; 2-(2-Methyl-5-nitroimidazol-1-yl)ethyl N-[2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl]carbamate; [2,2,2-trichloro-1-(2-pyrimidinylamino)ethyl]-carbamic acid, 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl ester
MSDS:
Inquire
InChIKey:
ZEXHXVOGJFGTRX-UHFFFAOYSA-N
InChI:
InChI=1S/C13H14Cl3N7O4/c1-8-19-7-9(23(25)26)22(8)5-6-27-12(24)21-10(13(14,15)16)20-11-17-3-2-4-18-11/h2-4,7,10H,5-6H2,1H3,(H,21,24)(H,17,18,20)
Canonical SMILES:
CC1=NC=C(N1CCOC(=O)NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)[N+](=O)[O-]
1.Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells.
Lub S;Maes A;Maes K;De Veirman K;De Bruyne E;Menu E;Fostier K;Kassambara A;Moreaux J;Hose D;Leleu X;King RW;Vanderkerken K;Van Valckenborgh E Oncotarget. 2016 Jan 26;7(4):4062-76. doi: 10.18632/oncotarget.6768.
The anaphase promoting complex/cyclosome (APC/C) is an ubiquitin ligase involved in cell cycle. During the metaphase-anaphase transition the APC/C is activated by Cdc20. The aim of this study is to elucidate the importance and therapeutic potential of APC/C and its co-activator Cdc20 in multiple myeloma (MM). Gene expression analysis revealed that Cdc20 was expressed at higher levels in gene expression-based high-risk MM patients. Moreover, high Cdc20 expression correlated with poor prognosis. Treatment of human myeloma cell lines with proTAME, an APC/C inhibitor, resulted in an accumulation of APC/CCdc20 substrate cyclin B1 and an accumulation of cells in metaphase. Moreover we observed a significant dose-dependent decrease in viability and increase in apoptosis in MM cells upon proTAME treatment. The induction of apoptosis was accompanied with caspase 3, 8, 9 and PARP cleavage. A similar metaphase arrest and induction of apoptosis were obtained with specific knockdown of Cdc20. In addition, we demonstrated the accumulation of Bim was partially responsible for the observed cell death. Combining proTAME with another APC/C inhibitor apcin or the alkylating agent melphalan resulted in enhanced anti-MM activity.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related APC Products


MAIT 203

MAIT 203 inhibits interaction of APC and Asef (RhoGEF4). It also inhibits colorectal cancer cell migration and invasion in vitro.

CAS 300815-04-7 Apcin

Apcin
(CAS: 300815-04-7)

Apcin is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C), which is a large multimeric complex. It functions a...

CAS 901-47-3 TAME

TAME
(CAS: 901-47-3)

TAME is a small molecule anaphase-promoting complex/cyclosome (APC) inhibitor.

CAS 331458-02-7 CFM 4

CFM 4
(CAS: 331458-02-7)

CFM 4 is a CARP-1 mimetic compound that inhibits CARP-1 binding to APC-2. It causes apoptosis and inhibition of cell growth in cancer cells.

CAS 1784-03-8 TAME hydrochloride

TAME hydrochloride
(CAS: 1784-03-8)

TAME hydrochloride is a competitive inhibitor of the anaphase-promoting complex/cyclosome (APC/C) and a synthetic substrate for thrombin, trypsin, plasminogen (...

Chemical Structure

CAS 300815-04-7 Apcin

Quick Inquiry

Verification code

Featured Items