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116805

Sigma-Aldrich

PKA Inhibitor 5-24

The PKA Inhibitor 5-24, also referenced under CAS 99534-03-9, controls the biological activity of PKA. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

PKA Inhibitor 5-24, Protein Kinase A Inhibitor 5-24, H-TTYADFIASGRTGRRNAIHD, PKA Inhibitor IV

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About This Item

Empirical Formula (Hill Notation):
C94H148N32O31
CAS Number:
Molecular Weight:
2222.38
MDL number:
UNSPSC Code:
12352200

Quality Level

Assay

≥95% (HPLC)

form

lyophilized

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)

solubility

water: 1 mg/mL

shipped in

ambient

storage temp.

−20°C

InChI

1S/C94H148N32O31/c1-11-42(3)70(124-85(150)58(31-50-19-14-13-15-20-50)117-84(149)61(35-67(135)136)116-74(139)44(5)110-81(146)57(32-51-24-26-53(131)27-25-51)119-90(155)73(49(10)130)126-86(151)69(96)47(8)128)88(153)112-45(6)75(140)122-63(40-127)77(142)107-38-65(133)114-55(22-17-29-105-93(99)100)80(145)125-72(48(9)129)87(152)108-39-66(134)113-54(21-16-28-104-92(97)98)78(143)115-56(23-18-30-106-94(101)102)79(144)118-60(34-64(95)132)82(147)111-46(7)76(141)123-71(43(4)12-2)89(154)120-59(33-52-37-103-41-109-52)83(148)121-62(91(156)157)36-68(137)138/h13-15,19-20,24-27,37,41-49,54-63,69-73,127-131H,11-12,16-18,21-23,28-36,38-40,96H2,1-10H3,(H2,95,132)(H,103,109)(H,107,142)(H,108,152)(H,110,146)(H,111,147)(H,112,153)(H,113,134)(H,114,133)(H,115,143)(H,116,139)(H,117,149)(H,118,144)(H,119,155)(H,120,154)(H,121,148)(H,122,140)(H,123,141)(H,124,150)(H,125,145)(H,126,151)(H,135,136)(H,137,138)(H,156,157)(H4,97,98,104)(H4,99,100,105)(H4,101,102,106)/t42-,43-,44-,45-,46-,47?,48?,49?,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,69-,70-,71-,72-,73-/m0/s1

InChI key

AXOXZJJMUVSZQY-BVDKBYOBSA-N

General description

A potent synthetic peptide that is a competitive inhibitor of protein kinase A (Ki = 2.3 nM). Its sequence is derived from the heat-stable skeletal muscle inhibitor protein of PKA. Binds to the catalytic subunit of PKA and displaces the regulatory subunit. Mimics the protein substrate by binding to the catalytic site via the arginine-cluster basic substrate.
Peptide corresponding to the active site on the skeletal muscle inhibitor protein. Competitive inhibitor of protein kinase A (Ki = 2.3 nM).

Biochem/physiol Actions

Cell permeable: no
Product does not compete with ATP.
Reversible: no
Target Ki: 2.3 nM for protein kinase A

Packaging

Yes

Warning

Toxicity: Standard Handling (A)

Sequence

H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-OH

Preparation Note

Sonication or the addition of a few drops of dilute acid (10 mM HCl) may be necessary to achieve complete solubilization.

Other Notes

Knighton, D.R., et al. 1991. Science 253, 525.
Cheng, H.C., et al. 1986. J. Biol. Chem. 261, 989.
Rusine, T., et al. 1986. J. Cell Biol.102, 1630.
Wong, Y.S., et al. 1986. J. Biol. Chem..261, 12089.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Determination of ERK activity: antiphospho-ERK antibodies, in vitro phosphorylation, and in-gel kinase assay.
Sarah Kraus et al.
Methods in molecular biology (Clifton, N.J.), 250, 29-48 (2004-02-03)

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