Calpain Inhibitor IA calpain and cathepsin inhibitor

Calpain Inhibitor I (CAS 110044-82-1)

Calpain Inhibitor I | CAS 110044-82-1 is rated 5.0 out of 5 by 1.
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Synonym: ALLN, Ac-LLnL-CHO, MG-101, N-Acetyl-Leu-Leu-Norleu-al, N-Acetyl-L-leucyl-L-leucyl-L-norleucinal
Application: A calpain and cathepsin inhibitor
CAS Number: 110044-82-1
Purity: ≥95%
Molecular Weight: 383.5
Molecular Formula: C20H37N3O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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Calpain Inhibitor I is an inhibitor of Calpain 1(calpain I) (Ki = 190 nM), Calpain 2(calpain II) (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. It also inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. Calpain Inhibitor I inhibits the proteolysis of IκBα and IκBβ by the ubiquitin-proteasome complex. Furthermore, it protects against neuronal damage caused by hypoxia and ischemia. Calpain Inhibitor I also prevents nitric oxide production by activated macrophages by interfering with transcription of the inducible nitric oxide synthase gene.


References

1. Sasaki, T., et al. 1990. J. Enzym. Inhib. 3: 195-201. PMID: 2079636
2. Sherwood, S.W., et al. 1993. Proc. Natl. Acad. Sci. U.S.A. 90: 3353-3357. PMID: 8386372
3. Squìer, M.K., et al. 1994. J. Cell. Physiol. 159: 229-237. PMID: 8163563
4. Lu, Q. and Mellgren, R.L. 1996. Arch. Biochem. Biophys. 334: 175-181. PMID: 8837753
5. Hoffman, L. and Rechsteiner, M. 1996. J. Biol. Chem. 271: 32538-32545. PMID: 8955078
6. Griscavage, J.M., et al. 1996. Proc. Natl. Acad. Sci. U.S.A. 93: 3308-3312. PMID: 8622934
7. Atencio, I.A., et al. 2000. Cell Growth Differ. 11: 247-253. PMID: 10845425
8. Chatterjee, P.K., et al. 2001. Kidney Int. 59: 2073-2083. PMID: 11380809
9. Perrin, C., et al. 2002. Cell. Mol. Biol. 48: OL267-OL270. PMID: 12643443

Usage :
Recommended working concentration: 17 μg/ml
Physical State :
Solid
Solubility :
Soluble in DMF, ethanol, and methanol. Insoluble in water.
Storage :
Store at 4° C
Melting Point :
267.52° C (Predicted)
Boiling Point :
~632.2° C at 760 mmHg (Predicted)
Density :
~1.0 g/cm3 (Predicted)
Refractive Index :
n20D 1.47 (Predicted)
IC50 :
proteasome: IC50 = 150 nM; L1210 : IC50 = 3 µM (mouse)
Ki Data :
calpain I: Ki= 190 nM; calpain II: Ki= 220 nM; cathepsin B: Ki= 150 nM; cathepsin L: Ki= 500 pM; neutral cysteine proteases and the proteasome: Ki= 6 µM
pK Values :
pKa: 13.53 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
443118
MDL Number :
MFCD00065505
Beilstein Registry :
7656053
SMILES :
CCCC[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)C

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Certificate of Analysis

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Calpain Inhibitor I  Product Citations

See how others have used Calpain Inhibitor I. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 26047104  Tang, F. et al. 2015. PloS one. 10: e0129128.

PMID: # 21276008  Datta, R. et al. 2011. Allergy. -.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Li SZ; et al Li SZ; et al. (PubMed ID: 25376843) determined that Calpain Inhibitor I decreased cell viability in UbcH10 deficient colorectal cancer cells. -SCBT Publication Review
Date published: 2015-01-30
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