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 (K_I(app)= 60 nM) and caspase-7 (K_I(app) = 170 nM). It is a weaker inhibitor of caspase-9 (K_I(app) = 3.1 μM). Caspase-3/7 Inhibitor I has only a trivial effect (K_i(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 :

n²⁰_D 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: K_i= 1100 nM (human); caspase-7: K_i= 170 nM; caspase-3: K_i= 60 nM

pK Values :

pK_a: 8.66 (Predicted)

仅供科研使用。不可用于诊断或治疗。

PubChem CID :

9840223

MDL Number :

MFCD22581511

SMILES :

COC[[email protected]@H]1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O

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