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Acetyl-Calpastatin (184-210) (human)

Calpain I/II inhibitor CAS# 123714-50-1

Acetyl-Calpastatin (184-210) (human)

Catalog No. BCC2350----Order now to get a substantial discount!

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Acetyl-Calpastatin (184-210) (human): 5mg $1840 In Stock
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Chemical structure

Acetyl-Calpastatin (184-210) (human)

3D structure

Chemical Properties of Acetyl-Calpastatin (184-210) (human)

Cas No. 123714-50-1 SDF Download SDF
PubChem ID 90488788 Appearance Powder
Formula C142H230N36O44S M.Wt 3177.65
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 5 mg/ml in water
Sequence DPMSSTYIEELGKREVTIPPKYRELLA

(Modifications: Asp-1 = N-terminal Ac, Ala-27 = C-terminal amide)

SMILES CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CCC(=O)O)C(=O)NC(CC(C)C)C(=O)NCC(=O)NC(CCCCN)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)O)C(=O)NC(C(C)C)C(=O)NC(C(C)O)C(=O)NC(C(C)CC)C(=O)N1CCCC1C(=O)N2CCCC2C(=O)NC(CCCCN)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)O)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)N)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(C(C)O)NC(=O)C(CO)NC(=O)C(CO)NC(=O)C(CCSC)NC(=O)C5CCCN5C(=O)C(CC(=O)O)NC(=O)C
Standard InChIKey ZXJCOYBPXOBJMU-HSQGJUDPSA-N
Standard InChI InChI=1S/C142H230N36O44S/c1-18-74(11)111(172-129(211)97(65-81-38-42-83(185)43-39-81)168-136(218)113(77(14)181)174-131(213)100(69-180)170-130(212)99(68-179)169-124(206)92(52-60-223-17)162-132(214)101-33-26-57-176(101)138(220)98(66-109(195)196)154-79(16)183)135(217)163-90(46-50-107(191)192)121(203)159-88(44-48-105(187)188)122(204)164-93(61-70(3)4)116(198)152-67-104(186)155-84(29-20-22-53-143)117(199)156-86(31-24-55-150-141(146)147)118(200)160-91(47-51-108(193)194)125(207)171-110(73(9)10)134(216)175-114(78(15)182)137(219)173-112(75(12)19-2)140(222)178-59-28-35-103(178)139(221)177-58-27-34-102(177)133(215)161-85(30-21-23-54-144)120(202)167-96(64-80-36-40-82(184)41-37-80)128(210)157-87(32-25-56-151-142(148)149)119(201)158-89(45-49-106(189)190)123(205)165-95(63-72(7)8)127(209)166-94(62-71(5)6)126(208)153-76(13)115(145)197/h36-43,70-78,84-103,110-114,179-182,184-185H,18-35,44-69,143-144H2,1-17H3,(H2,145,197)(H,152,198)(H,153,208)(H,154,183)(H,155,186)(H,156,199)(H,157,210)(H,158,201)(H,159,203)(H,160,200)(H,161,215)(H,162,214)(H,163,217)(H,164,204)(H,165,205)(H,166,209)(H,167,202)(H,168,218)(H,169,206)(H,170,212)(H,171,207)(H,172,211)(H,173,219)(H,174,213)(H,175,216)(H,187,188)(H,189,190)(H,191,192)(H,193,194)(H,195,196)(H4,146,147,150)(H4,148,149,151)/t74-,75-,76-,77+,78+,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,110-,111-,112-,113-,114-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Acetyl-Calpastatin (184-210) (human)

DescriptionSelective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 μM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio.

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Background on Acetyl-Calpastatin (184-210) (human)

Selective calpain inhibitor. Strongly inhibits calpain I (Ki = 0.2 nM) and II but does not inhibit papain, trypsin and cathepsin L (Ki = 6 μM). Increases secretion of amyoid β-protein (Aβ) 42, Aβ40 and Aβ42 ratio.

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References on Acetyl-Calpastatin (184-210) (human)

Inhibition of calpain by a synthetic oligopeptide corresponding to an exon of the human calpastatin gene.[Pubmed:2553724]

J Biol Chem. 1989 Nov 15;264(32):18866-9.

Calpastatin is a widely distributed endogenous inhibitor protein specifically acting on calpain (Ca2+-dependent cysteine endopeptidase). The inhibitor consists of four inhibitory domains (Domains 1-4) with mutually homologous sequences. NH2-terminal Domain L is non-homologous, and all domains have 120-140 residues each. A human calpastatin genomic DNA clone was isolated using a previously obtained human calpastatin cDNA probe. Sequence analysis has revealed that the clone contains Domain 1 and segments of neighboring domains (Domains L and 2). Each of three highly conserved, restricted regions within Domain 1 was located on separate exons, 1A, 1B, and 1C. Exon 2A, corresponding to the first exon of Domain 2, is homologous to Exon 1A and follows Exon 1D of Domain 1. A 27-residue peptide encoded by Exon 1B, including a 12-residue middle conserved sequence, was chemically synthesized and tested for protease inhibitory activities. The synthetic peptide showed strong inhibition against calpain I (low Ca2+-requiring form), and calpain II (high Ca2+-requiring form), but no inhibition against papain or trypsin. These results indicated that Exon 1B forms a self-sufficient functional subdomain of the calpastatin inhibitory domain.

Description

Selective calpain inhibitor

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