Apcin


Catalog No. Size PriceQuantity
M7536-2 2mg solid $205
M7536-10 10mg solid $820

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.

Product information

CAS Number: 300815-04-7

Molecular Weight: 438.65

Formula: C13H14Cl3N7O4

Chemical Name: 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl (2,2,2-trichloro-1-(pyrimidin-2-ylamino)ethyl)carbamate

Smiles: CC1=NC=C(N1CCOC(=O)NC(NC1N=CC=CN=1)C(Cl)(Cl)Cl)[N+]([O-])=O

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 88 mg/mL (200.62 mM) Ethanol 10 mg/mL (22.80 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. The inhibition of CDC20 with its inhibitor Apcin reduces the adhesion rate and proliferation ability to RL95-2 and HEC-1A cells, respectively.

In Vivo:

CDC20 inhibitor Apcin inhibits embryo implantation in vivo.

References:

  1. Katharine L Sackton, et al. Nature. 2014 Oct 30;514(7524):646-9.
  2. Yuan Gao, et al. Oncol Rep. 2018 Aug;40(2):841-848.
  3. Chuanjia Guo, et al. Cell Biochem Funct. 2020 Aug;38(6):810-81

Products are for research use only. Not for human use.

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