TAT-cyclo-CLLFVY is a selective HIF-1 dimerization inhibitor. TAT-cyclo-CLLFVY blocks protein-protein interaction of recombinant HIF-1α, but not HIF-2α, with HIF-1β (IC50=1.3 μM). TAT-cyclo-CLLFVY inhibits hypoxia-induced HIF-1 activity and decreases VEGF and CAIX expression in osteosarcoma and breast cancer cells in vitro. TAT-cyclo-CLLFVY also reduces the tubularization of hypoxic HUVECs.
CAT No: GR1228
CAS No: 1446322-66-2
Synonyms/Alias: TAT-cyclo-CLLFVY;1446322-66-2;TAT-cyclo-CLLFVY TFA;AKOS027470216;DA-58295;PD079835;
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M.F/Formula | C111H188N42O24S2 |
M.W/Mr. | 2559.1 |
Sequence | One Letter Code:CGRKKRRQRRRPPQ Three Letter Code:H-Cys(1)-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Pro-Pro-Gln-OH.cyclo[Cys(1)-Leu-Leu-Phe-Val-Tyr] |
Purity | >98 % |
Long-term Storage Conditions | Soluble to 1 mg/ml in water |
Shipping Condition | +20°C (International: -20°C) |
InChI | InChI=1S/C111H188N42O24S2/c1-59(2)52-76-97(168)148-79(54-62-22-8-7-9-23-62)99(170)151-86(61(5)6)102(173)149-78(55-63-34-36-64(154)37-35-63)98(169)150-80(100(171)147-77(53-60(3)4)96(167)146-76)58-179-178-57-65(114)87(158)135-56-85(157)136-66(26-14-44-129-106(117)118)88(159)137-67(24-10-12-42-112)89(160)138-68(25-11-13-43-113)90(161)139-69(27-15-45-130-107(119)120)91(162)140-71(29-17-47-132-109(123)124)93(164)143-73(38-40-83(115)155)95(166)142-70(28-16-46-131-108(121)122)92(163)141-72(30-18-48-133-110(125)126)94(165)144-74(31-19-49-134-111(127)128)103(174)153-51-21-33-82(153)104(175)152-50-20-32-81(152)101(172)145-75(105(176)177)39-41-84(116)156/h7-9,22-23,34-37,59-61,65-82,86,154H,10-21,24-33,38-58,112-114H2,1-6H3,(H2,115,155)(H2,116,156)(H,135,158)(H,136,157)(H,137,159)(H,138,160)(H,139,161)(H,140,162)(H,141,163)(H,142,166)(H,143,164)(H,144,165)(H,145,172)(H,146,167)(H,147,171)(H,148,168)(H,149,173)(H,150,169)(H,151,170)(H,176,177)(H4,117,118,129)(H4,119,120,130)(H4,121,122,131)(H4,123,124,132)(H4,125,126,133)(H4,127,128,134)/t65-,66-,67-,68-,69-,70-,71-,72-,73-,74-,75-,76-,77-,78-,79-,80-,81-,82-,86-/m0/s1 |
InChI Key | AWUUHEHYNQGEFC-XLZVTALKSA-N |
Canonical SMILES | CC(C)CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC(C)C)CSSCC(C(=O)NCC(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCNC(=N)N)C(=O)N2CCCC2C(=O)N3CCCC3C(=O)NC(CCC(=O)N)C(=O)O)N)CC4=CC=C(C=C4)O)C(C)C)CC5=CC=CC=C5 |
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