Free shipping on all orders over $ 500

MG-101

Cat. No. M5221
MG-101 Structure
Synonym:

Calpain inhibitor-1

Size Price Availability
5mg USD 87  USD87 Custom Synthesis
10mg USD 135  USD135 Custom Synthesis
50mg USD 450  USD450 Custom Synthesis
100mg USD 723  USD723 Custom Synthesis
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MG-101 is an inhibitor of Calpain 1 (Ki = 190 nM), Calpain 2 (Ki = 220 nM), cathepsin B (Ki = 150 nM), and cathepsin L (Ki = 500 pM). It inhibits neutral cysteine proteases and proteasome (Ki = 6 μM). It inhibits apoptosis in thymocytes and metamyelocytes. MG-101 also inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. MG-101 inhibits the proteolysis of IκBα and IκBβ by the ubiquitin-proteasome complex. Furthermore, it protects against neuronal damage caused by hypoxia and ischemia. MG-101 also prevents nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene.

Protocol
Cell Experiment
Cell lines HCT116,HCT116/p53−/−,和 HCT116/Bax−/−
Preparation method Cells viability is assayed using Cell Counting Kit-8 following manufacturer’s protocol. All HCT116 cell typesare seeded into each well of 96-well plate, cultured to 80% density and treated with different doses of ALLN for 24 h. Medium is then replaced by 100 μl fresh McCoy’s 5A complete medium with 10% CCK-8 reagent and incubated for 1 h. Absorbance is measured at 450 nm using a microplate reader. Results are shown as death percentages.
Concentrations ~26 μM
Incubation time 24h
Animal Experiment
Animal models Female athymic nude mice bearing HCT116 xenografts
Formulation Saline
Dosages 10 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 383.53
Formula C20H37N3O4
CAS Number 110044-82-1
Purity >98%
Solubility 76mg/ml in DMSO
Storage at -20°C
References

[1] Li SZ, et al. Biochem Biophys Res Commun. ALLN hinders HCT116 tumor growth through Bax-dependent apoptosis.

[2] Hiwasa, et al. Carcinogenesis. Cysteine proteinase inhibitors and ras gene products share the same biological activities including transforming activity toward NIH3T3 mouse fibroblasts and the differentiation-inducing activity toward PC12 rat pheochromocytoma cells.

Related Proteasome Products
RA190 hydrochloride

RA190 HCl is a potent RPN13 and ADRM1 Inhibitor, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

PTP1B-IN-9

PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor with anticancer activity.

MDL 28170

MDL 28170 is a potent cell permeable calpain I and II inhibitor, it reduces capsaicin-mediated cell death in cultured dorsal root ganglion neurons.

Sivelestat sodium tetrahydrate

Sivelestat sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

VR23

VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3 μM).

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MG-101, Calpain inhibitor-1 supplier, Proteasome, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.