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G7923 Sigma-Aldrich

GO-201 trifluoroacetate salt

≥95% (HPLC)

Synonym: D-Arg-D-Arg- D-Arg- D-Arg- D-Arg- D-Arg- D-Arg- D-Arg- D-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn-Tyr-Gly-Gln-Leu-Asp-Ile-Phe-Pro trifluoroacetate

  • Empirical Formula (Hill Notation) C133H233N61O31S2 · xC2HF3O2

  • Molecular Weight 3246.79 (free base basis)

  •  MDL number MFCD18452843

  •  PubChem Substance ID 329799971

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Properties

Related Categories Apoptosis Inducers, Apoptosis and Cell Cycle, Cell Biology, Cell Signaling and Neuroscience
assay   ≥95% (HPLC)
form   lyophilized
color   white
solubility   H2O: >1 mg/mL
storage temp.   −20°C
SMILES string   OC(=O)C(F)(F)F.CC[C@H](C)[C@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CS)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@@H](CCCNC(N)=N)NC(=O)[C@H](N)CCCNC(N)=N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N3CCC[C@H]3C(O)=O
InChI   1S/C133H233N61O31S2.C2HF3O2/c1-5-68(4)99(120(222)190-90(61-69-23-7-6-8-24-69)121(223)194-58-22-37-93(194)122(224)225)193-117(219)89(63-98(200)201)189-115(217)86(59-67(2)3)186-113(215)84(42-44-94(136)196)173-97(199)64-172-101(203)87(60-70-38-40-71(195)41-39-70)187-116(218)88(62-96(138)198)188-111(213)73(26-9-10-46-134)175-103(205)75(28-13-49-163-125(143)144)182-110(212)82(35-20-56-170-132(157)158)184-118(220)91(65-226)192-114(216)85(43-45-95(137)197)185-119(221)92(66-227)191-112(214)83(36-21-57-171-133(159)160)183-109(211)81(34-19-55-169-131(155)156)181-108(210)80(33-18-54-168-130(153)154)180-107(209)79(32-17-53-167-129(151)152)179-106(208)78(31-16-52-166-128(149)150)178-105(207)77(30-15-51-165-127(147)148)177-104(206)76(29-14-50-164-126(145)146)176-102(204)74(27-12-48-162-124(141)142)174-100(202)72(135)25-11-47-161-123(139)140;3-2(4,5)1(6)7/h6-8,23-24,38-41,67-68,72-93,99,195,226-227H,5,9-22,25-37,42-66,134-135H2,1-4H3,(H2,136,196)(H2,137,197)(H2,138,198)(H,172,203)(H,173,199)(H,174,202)(H,175,205)(H,176,204)(H,177,206)(H,178,207)(H,179,208)(H,180,209)(H,181,210)(H,182,212)(H,183,211)(H,184,220)(H,185,221)(H,186,215)(H,187,218)(H,188,213)(H,189,217)(H,190,222)(H,191,214)(H,192,216)(H,193,219)(H,200,201)(H,224,225)(H4,139,140,161)(H4,141,142,162)(H4,143,144,163)(H4,145,146,164)(H4,147,148,165)(H4,149,150,166)(H4,151,152,167)(H4,153,154,168)(H4,155,156,169)(H4,157,158,170)(H4,159,160,171);(H,6,7)/t68-,72+,73-,74+,75-,76+,77+,78+,79+,80+,81+,82-,83+,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,99-;/m0./s1
InChI key   MDUBLMWNQKKWEW-VECPGXDMSA-N

Description

General description

GO-201 is a synthetic peptide, which functions as an inhibitor of MUC1 (mucin1) oncoprotein. It corresponds to the cytoplasmic domain of MUC1, MUC1-CD (1-15).

Application

GO-201 trifluoroacetate salt has been used as a drug for the treatment of K562 cells transfected with CCmut2 (coiled-coil mutant), to determine the overall effect on the proliferative capacity of K562 cells.

Packaging

1 mg in glass bottle

Biochem/physiol Actions

GO-201 binds with the cytoplasmic domain of MUC1 (mucin 1) protein, thus preventing the oligomerization of MUC1 protein in cells. In human breast cancer cells, this peptide prevents the transport of MUC1 to nucleus, causes disruption of redox equilibrium and induces DNA damage response. It prevents the interaction between NFκB (nuclear factor) and MUC1, thus, preventing activation of MUC1 by NFκB. GO-201 suppresses the expression of the anti-apoptotic protein Bcl-xL (B-cell lymphoma-extra large). This peptide also inhibits growth and initiates death by necrosis. Studies in nude mice with human breast tumor xenograts, show that the use of GO-201 results in massive necrosis and intensive regression of tumorigenesis.

GO-201 is a mucin1 (MUC1) inhibitor that binds to the MUC1-C CQC motif and directly blocks MUC1function, inhibits cell proliferation, and induces necrotic cell death in MUC1-positive cell lines. The mucin 1 (MUC1) oncoprotein is aberrantly expressed at high levels in human carcinomas. MUC1 is heterodimer that consists of NH2-terminal (MUC1-N) and COOH-terminal (MUC1-C) subunits. Overexpression of MUC1 blocks the induction of apoptosis and necrosis in the cellular response to DNA-damaging agents, reactive oxygen species, hypoxia ,and glucose deprivation. GO-201 is an inhibitor of MUC1, which interacts directly with the MUC1-C subunit at its oligomerization domain. The compound inhibits cell proliferation and induces necrotic cell death in of MUC1-positive cell lines ant grafts.

GO-201 is a mucin1 (MUC1) inhibitor that binds to the MUC1-C CQC motif and directly blocks MUC1function, inhibits cell proliferation, and induces necrotic cell death in MUC1-positive cell lines.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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