Caspase-3/7 Inhibitor I Caspase-3/7 Inhibitor I is an inhibitor of caspase-3, caspase-7 and Caspase-9.

Caspase-3/7 Inhibitor I (CAS 220509-74-0)

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Alternate Names: 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
Application: Caspase-3/7 Inhibitor I is an inhibitor of caspase-3, caspase-7 and Caspase-9
CAS Number: 220509-74-0
Purity: ≥98%
Molecular Weight: 324.4
Molecular Formula: C14H16N2O5S
仅供科研使用。不可用于诊断或治疗。
* 参考分析证明 大量特定数据 (包括水 含量).
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Caspase-3/7 Inhibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app)= 60 nM) and caspase-7 (KI(app) = 170 nM). It is a weaker inhibitor of caspase-9 (KI(app) = 3.1 μM). Caspase-3/7 Inhibitor I has only a trivial effect (Ki(app) >25 μM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. It has been shown to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 μM). Caspase-3/7 Inhibitor I has also been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 μM and 98% inhibition at 50 μM). Selectivity for caspases 3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue.


参考文献

1. Lee, D., et al. 2000. J. Biol. Chem. 275: 16007-16014. PMID: 10821855
2. Lee, D., et al. 2001. J. Med. Chem. 44: 2015-2026. PMID: 11384246
3. Lührmann, Anja., et al., 2004. Necrotic death of Rhodococcus equi-infected macrophages is regulated by virulence-associated plasmids. Infection and immunity. 72(2): 853-62. PMID: 14742529

Physical State :
Solid
Solubility :
Soluble in DMSO (200 mg/ml), and methanol (10 mg/ml).
Storage :
Store at -20° C
Melting Point :
228.25° C (Predicted)
Boiling Point :
533.50° C (Predicted)
Density :
1.42 g/cm3 (Predicted)
Refractive Index :
n20D 1.60 (Predicted)
IC50 :
caspase-7: IC50 = 170 nM (human); caspase-3: IC50 = 84.9 nM (human); apoptosis: IC50 = ~50 µM (camptothecin treated Jurkat cells)
Ki Data :
Caspase-9: Ki= 1100 nM (human); caspase-7: Ki= 170 nM; caspase-3: Ki= 60 nM
pK Values :
pKa: 8.66 (Predicted)
仅供科研使用。不可用于诊断或治疗。
PubChem CID :
MDL Number :
MFCD22581511
SMILES :
COC[[email protected]@H]1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O

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Citations 1 to 4 of 4 total

PMID: # 24587248  Wang, J. et al. 2014. PLoS ONE. 9: e90146.

PMID: # 23658722  Boehm, D. et al. 2013. PLoS ONE. 8: e62303.

PMID: # 22335196  Wang, J. et al. 2012. J. Pineal Res. 53: 77-90.

PMID: # 32345661  Life Sci Alliance. 3:

Citations 1 to 4 of 4 total
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