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
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
H-Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp-OH
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
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| 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 |
| SMILES string | [nH]1cnc(c1)C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](N)C(O)C)C(O)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 |
