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G7923

Sigma-Aldrich

GO-201 trifluoroacetate salt

≥95% (HPLC)

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Synonym(s):
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

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

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.

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.
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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Deepak Raina et al.
Cancer research, 69(12), 5133-5141 (2009-06-06)
The mucin 1 (MUC1) oncoprotein is aberrantly overexpressed by approximately 90% of human breast cancers. However, there are no effective agents that directly inhibit MUC1 and induce death of breast cancer cells. We have synthesized a MUC1 inhibitor (called GO-201)
David W Woessner et al.
Molecular pharmaceutics, 10(1), 270-277 (2012-12-06)
Chronic myeloid leukemia (CML) is a myeloproliferative disorder caused by expression of the fusion gene BCR-ABL following a chromosomal translocation in the hematopoietic stem cell. Therapeutic management of CML uses tyrosine kinase inhibitors (TKIs), which block ABL-signaling and effectively kill
Rehan Ahmad et al.
Cancer research, 69(17), 7013-7021 (2009-08-27)
Nuclear factor-kappaB (NF-kappaB) is constitutively activated in diverse human malignancies. The mucin 1 (MUC1) oncoprotein is overexpressed in human carcinomas and, like NF-kappaB, blocks cell death and induces transformation. The present studies show that MUC1 constitutively associates with NF-kappaB p65

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