General description
A 26-residue polypeptide from bee venom that binds calmodulin in a Ca2+-dependent manner, activates phospholipase A2, and inhibits protein kinase C (IC50 = 5-7 µM) by binding to the catalytic domain in a Mg2+-ATP sensitive manner. A stimulator of Giα and G11α activity that is reported to inhibit adenylate cyclase activity in synaptic membranes. Has also been used for affinity purification of several Ca2+-binding proteins. Activates Giα-1 and G11α activities and inhibits Gs activity.
Biochem/physiol Actions
Cell permeable: no
Product does not compete with ATP.
Reversible: no
Target IC50: 5-7 µM 5-7 µM for activating phospholipase A2 and inhibits protein kinase C
Packaging
Yes
Other Notes
Fukushima, N., et al. 1998. Peptides19, 811.
Gravitt, K.R. 1994. Biochem. Pharmacol. 47, 425.
Baudier, J., et al. 1987. Biochemistry26, 2886.
Kincaid, R.L., and Coulson, C.C. 1985. Biochem. Biophys. Res. Commun.133, 256.
H-Gly-Ile-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly-Leu-Pro-Ala-Leu-Ile-Ser-Trp-Ile-Lys-Arg-Lys-Arg-Gln-Gln-NH₂
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| description | Merck USA index - 14, 5824 |
| assay | >97% (HPLC) |
| form | lyophilized |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| solubility | water: 1 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | N1(C(CCC1)C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(C(CC)C)C(=O)NC(CO)C(=O)NC(Cc2c3c([nH]c2)cccc3)C(=O)NC(C(CC)C)C(=O)NC(CCCCN)C(=O)NC(CCCN\C(=N\[H])\N)C(=O)NC(CCCCN)C(=O)NC(CCCN\C(=N\[H])\N)C(=O)NC(CCC(=O)N)C(=O)NC(CCC(=O)N)C(=O)N)C(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC |
| InChI | 1S/C131H229N39O31/c1-23-71(16)102(163-97(176)60-135)122(194)146-62-98(177)148-74(19)109(181)164-100(69(12)13)124(196)160-88(55-65(4)5)116(188)155-84(41-30-33-51-134)115(187)165-101(70(14)15)125(197)161-90(57-67(8)9)118(190)168-106(77(22)173)128(200)169-105(76(21)172)123(195)147-63-99(178)150-92(58-68(10)11)129(201)170-54-36-44-94(170)121(193)149-75(20)108(180)158-89(56-66(6)7)117(189)166-104(73(18)25-3)127(199)162-93(64-171)120(192)159-91(59-78-61-145-80-38-27-26-37-79(78)80)119(191)167-103(72(17)24-2)126(198)157-83(40-29-32-50-133)111(183)154-85(42-34-52-143-130(139)140)112(184)152-82(39-28-31-49-132)110(182)153-86(43-35-53-144-131(141)142)113(185)156-87(46-48-96(137)175)114(186)151-81(107(138)179)45-47-95(136)174/h26-27,37-38,61,65-77,81-94,100-106,145,171-173H,23-25,28-36,39-60,62-64,132-135H2,1-22H3,(H2,136,174)(H2,137,175)(H2,138,179)(H,146,194)(H,147,195)(H,148,177)(H,149,193)(H,150,178)(H,151,186)(H,152,184)(H,153,182)(H,154,183)(H,155,188)(H,156,185)(H,157,198)(H,158,180)(H,159,192)(H,160,196)(H,161,197)(H,162,199)(H,163,176)(H,164,181)(H,165,187)(H,166,189)(H,167,191)(H,168,190)(H,169,200)(H4,139,140,143)(H4,141,142,144) |
| InChI key | VDXZNPDIRNWWCW-UHFFFAOYSA-N |
