Home Ubiquitin E3 Ligase inhibitor - APC inhibitor - CDK inhibitor Apcin For research use only.

Apcin

Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.

Apcin Chemical Structure

Apcin Chemical Structure

CAS: 300815-04-7

Selleck's Apcin has been cited by 3 publications

Purity & Quality Control

Batch: S960501 DMSO] 88 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false Purity: 99.49%
99.49

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Biological Activity

Description Apcin (APC inhibitor) is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C) that binds to Cdc20 and competitively inhibits the ubiquitylation of D-box-containing substrates.
Targets
APC/C [1] CDC20 [1]
In vitro
In vitro

Apcin is a novel cell‑permeable molecule that blocks the interaction between APC/C and Cdc20. Apcin is demonstrated to inhibit OS cell growth and induce significant apoptosis. The invasion and mobile abilities of OS cells are also markedly suppressed by apcin treatment. Furthermore, Bim and p21 are upregulated in OS cells following apcin treatment.[2] The inhibition of CDC20 with its inhibitor Apcin reduces the adhesion rate and proliferation ability to RL95-2 and HEC-1A cells, respectively.[3]
Cell Research Cell lines Human osteosarcoma cell lines MG63 and U2OS
Concentrations 25 μM, 50 μM, 75 μM
Incubation Time 24 h, 48 h, 72 h
Method

MG63 and U2OS (2.5×103 cells/well) are seeded in 96‑well plates and cultured overnight. Different concentrations of apcin are added to the medium and cultured for 24, 48 and 72 h, respectively. An MTT assay is then carried out to assess the cell viability according to the manufacturer's protocols. Then, 10 μl of MTT solution (0.5 mg/ml) is added to each well followed by incubation for 4 h. The liquid supernatant is then drained off and 100 μl of DMSO is added to each well to dissolve the crystals. The absorbance of each well at 490 nm is determined using a Multimode Reader of SpectraMax M5.
In Vivo
In vivo

CDC20 inhibitor Apcin inhibits embryo implantation in vivo.[3]
Animal Research Animal Models 8-week-old adult C57BL/6 female mice (weighing 20 to 25 g), 12-week-old adult C57BL/6 male mice (weighing 40 to 50 g)
Dosages --
Administration Uterine horn injection

Chemical Information & Solubility

Molecular Weight 438.65 Formula

C13H14Cl3N7O4
CAS No. 300815-04-7 SDF --
Smiles CC1=NC=C(N1CCOC(=O)NC(C(Cl)(Cl)Cl)NC2=NC=CC=N2)[N+](=O)[O-]
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 88 mg/mL ( (200.61 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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