PEPS-RO

Pepstatin

from Streptomyces species

• 동의어(들): Pepstatin A
• 실험식(Hill 표기법): C₃₄H₆₃N₅O₉
• CAS Number: 26305-03-3
• Molecular Weight: 685.89
• 효소 위원회 번호: 3.4.14.9 (BRENDA, IUBMB)
• Beilstein: 2201362
• MDL number: MFCD00060740
• UNSPSC 코드: 12352202
• PubChem Substance ID: 329820361

속성

• 생물학적 소스: synthetic
• Quality Level: 100
• 형태: lyophilized
• 포장: pkg of 10 mg (11359053001); pkg of 2 mg (10253286001); pkg of 50 mg (11524488001)
• 제조업체/상표: Roche
• 기술: affinity chromatography: suitable; protein purification: suitable
• mp: 233 °C (dec.) (lit.)
• solubility: ethanol: 1 mg/mL; methanol: 1 mg/mL; acetic acid: soluble 300 μg/mL (6N); pyridine: soluble; water: insoluble
• 저장 온도: 2-8°C
• SMILES string: CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)C[C@H](O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CC(C)C)C(C)C)C(C)C)[C@@H](O)CC(O)=O
• InChI: 1S/C34H63N5O9/c1-17(2)12-23(37-33(47)31(21(9)10)39-34(48)30(20(7)8)38-27(42)14-19(5)6)25(40)15-28(43)35-22(11)32(46)36-24(13-18(3)4)26(41)16-29(44)45/h17-26,30-31,40-41H,12-16H2,1-11H3,(H,35,43)(H,36,46)(H,37,47)(H,38,42)(H,39,48)(H,44,45)/t22-,23-,24-,25-,26-,30-,31-/m0/s1
• InChI key: FAXGPCHRFPCXOO-LXTPJMTPSA-N

설명

일반 설명

Isovaleryl-L-val-L-val-statyl-L-alanyl-statin (Isovaleryl-L-val-L-val-4-(S)-amino-3-(S)-hydroxy-6-methyl-heptanoyl-2-ala-4-(S)-amino-3-(S)-hydroxy-6-methyl-heptanoic acid)
Pepstatin is a low molecular weight, highly specific inhibitor of acid proteases (in particular aspartate proteases).

특이성

Pepstatin potently inhibits the HIV protease and other aspartic proteases, such as pepsin, renin, cathepsin D, chymosin, protease B from Aspergillus niger, and acid proteases of microbial origin.

애플리케이션

Pepstatin is used for the protection of proteins and enzymes during isolation and purification procedures. It facilitates the investigation of enzyme mechanisms and biological function, and the classification of proteases. Pepstatin is applied in affinity chromatography, structural and pharmacological research, in HIV research (inhibition of retroviral-coded proteases, e.g., HIV-1), and cancer research (as an immunostimulant and anti-tumor drug).

생화학적/생리학적 작용

Pepstatin A is an inhibitor of acid proteases (aspartyl peptidases). It forms a 1:1 complex with proteases such as pepsin, renin, cathepsin D, bovine chymosin, and protease B (Aspergillus niger). The inhibitor is highly selective and does not inhibit thiol proteases, neutral proteases, or serine proteases. Solubilized γ-secretase and retroviral protease are also inhibited by Pepstatin A. It has been used to characterize proteases from several sources.

품질

Purity tested by HPLC.

제조 메모

Working concentration: 0.7 μg/ml (1 μM)
Working solution: Recommended solvent is methanol (1 mg/ml), ethanol, DMSO or glacial acetic acid.
Pepstatin is insoluble in pure water, but it is possible to produce an aqueous solutions with methanol (1.5–2.0 mg/ml), ethanol (1 mg/ml if allowed to sit overnight) or DMSO. Pepstatin is also soluble in acetic acid (6 N, 300 μg/ml) and pyridine. Solubility in NaCl solution is not known. Sodium or magnesium salts of pepstatin are water-soluble.
Stock solution: 1.4 mg pepstatin/mI (2 mM), in methanol
Storage conditions (working solution): -15 to -25 °C

Pepstatin can be dissolved at 1 mg/ml in 10% (v/v) acetic acid in methanol (9:1 methanol:acetic acid). The inclusion of acetic acid may be necessary to dissolve this peptide in methanol or DMSO. It has been dissolved at 1 to 2 mg/ml in ethanol, but heat may be required for complete dissolution. Solutions of Pepstatin A can be heated as high as 60 °C without any decomposition of the peptide.
Stock solutions at 1 mg/ml are stable at least a week at 4 °C. A 1 mM solution in methanol or DMSO is stable for months at -20 °C. If solutions become darker yellow, the reagent is hydrolyzing.
A working concentration of 1 μM is stable for at least one day at room temperature.

재구성

Soluble in methanol to approximately 1 mg/ml. Also soluble to 1 mg/ml in ethanol if allowed to sit overnight, and to 300 μg/ml in 6 N acetic acid. Stable for at least one week at 2 to 8 °C, or one month when stored in aliquots at -15 to -25 °C.

기타 정보

For life science research only. Not for use in diagnostic procedures.

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable