Apcin

Modify Date: 2025-08-25 15:54:04

Apcin structure	Common Name	Apcin
	CAS Number	300815-04-7	Molecular Weight	438.65400
	Density	1.68±0.1 g/cm3	Boiling Point	N/A
	Molecular Formula	C₁₃H₁₄Cl₃N₇O₄	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A
	Symbol	GHS07	Signal Word	Warning

Use of Apcin

Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis[1][2][3].

Name	apcin
Synonym	More Synonyms

Description	Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis[1][2][3].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> APC
In Vitro	Apcin (25-50 μM; 48 hours) significantly increases MM apoptosis combining with proTAME (6, 12 μM)[3]. Apcin (25 μM; 2-14 hours) induces slippage more slowly[2]. Apcin (50-200 μM) stabilizes cycB1-NT and securin most effectively, with somewhat weaker effects against full-length cyclin B1[1]. Apcin (1.5-200 μM; 18 hours) synergizes with proTAME (a cell-permeable TAME prodrug) to prolong mitotic duration in RPE1 cells[1]. Apoptosis Analysis[3] Cell Line: HMCLs LP-1 and RPMI-8226 cells Concentration: 25, 50 μM Incubation Time: 48 hours Result: Had minor effects on multiple myeloma (MM) cells alone and significantly increased MM apoptosis combining with proTAME (6, 12 μM). Western Blot Analysis[2] Cell Line: HeLa cells with Nocodazole (100 nM) Concentration: 25 μM Incubation Time: 2-14 hours Result: Induced slippage more slowly, as indicated by Cdc27 dephosphorylation and a reduction in cyclin B1, securin and phosphoH3 levels beginning 4-6h after mitotic entry.
References	[1]. Katharine L Sackton, et al. Synergistic blockade of mitotic exit by two chemical inhibitors of the APC/C. Nature. 2014 Oct 30;514(7524):646-9. [2]. Katherine V Richeson, et al. Paradoxical mitotic exit induced by a small molecule inhibitor of APC/C Cdc20. Nat Chem Biol. 2020 May;16(5):546-555. [3]. Susanne Lub, et al. Inhibiting the anaphase promoting complex/cyclosome induces a metaphase arrest and cell death in multiple myeloma cells. Oncotarget. 2016 Jan 26;7(4):4062-76.

Density	1.68±0.1 g/cm3
Molecular Formula	C₁₃H₁₄Cl₃N₇O₄
Molecular Weight	438.65400
Exact Mass	437.01700
PSA	139.78000
LogP	3.41140
InChIKey	ZEXHXVOGJFGTRX-UHFFFAOYSA-N
SMILES	Cc1ncc([N+](=O)[O-])n1CCOC(=O)NC(Nc1ncccn1)C(Cl)(Cl)Cl

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P305 + P351 + P338
Hazard Codes	Xi
RIDADR	NONH for all modes of transport

Name: Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated fo...
Source: ChEMBL
Target: HeLa
External Id: CHEMBL4406125

Name: Cytotoxicity in human OVCAR3 cells assessed as reduction in cell viability incubated ...
Source: ChEMBL
Target: OVCAR-3
External Id: CHEMBL4406126

Name: Cytotoxicity in human Caov3 cells assessed as reduction in cell viability incubated f...
Source: ChEMBL
Target: Caov-3 cell line
External Id: CHEMBL4406127

Name: Binding affinity to CDC20 (unknown origin) by SPR analysis
Source: ChEMBL
Target: Cell division cycle protein 20 homolog
External Id: CHEMBL4406128

Name: Inhibition of CDC20 in human HepG2 cells assessed as increase in Bim protein levels a...
Source: ChEMBL
Target: Cell division cycle protein 20 homolog
External Id: CHEMBL4406130

Name: Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated fo...
Source: ChEMBL
Target: MCF7
External Id: CHEMBL4406121

Name: Cytotoxicity in human A375 cells assessed as reduction in cell viability incubated fo...
Source: ChEMBL
Target: A-375
External Id: CHEMBL4406122

Name: Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated fo...
Source: ChEMBL
Target: A549
External Id: CHEMBL4406123

Name: Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated f...
Source: ChEMBL
Target: HepG2
External Id: CHEMBL4406124

Name: Cell cycle arrest in human MDA-MB-231 cells assessed as G2 phase cells at 100 uM incu...
Source: ChEMBL
Target: MDA-MB-231
External Id: CHEMBL5507395

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Apcin

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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.