GO-201三氟乙酸盐，GO-201 trifluoroacetate salt；≥95% (HPLC)

图片 GO-201三氟乙酸盐，GO-201 trifluoroacetate salt；≥95% (HPLC)
别名：GO201 TFA；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 经验公式（希尔记法）: C133H233N61O31S2 · xC2HF3O2 分子量: 3246.79 (free base basis) MDL编号: MFCD18452843 PubChem化学物质编号: 329799971
制造商品牌: 西格玛 Sigma-Aldrich
货号（SKU）: G7923
MDL号: MFCD18452843
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¥3,493.96

说明

一般描述

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).[1][2]
 

应用

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.[3]
 

生化/生理作用

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.[1][2]
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.
 
 

属性

质量水平

100

检测方案

≥95% (HPLC)

形式

lyophilized

颜色

white

溶解性

H2O: >1 mg/mL

储存温度

−20°C

SMILES字符串

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

 

安全信息

储存分类代码

11 - Combustible Solids

WGK

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 50 | 欧洲Eur. ≥ 12 | 東京Tokyo ≥ 20 | 香港与北京 ≥ 50
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