G7923

GO-201 trifluoroacetate salt

≥95% (HPLC)

• 同義詞: 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
• 經驗公式（希爾表示法）: C₁₃₃H₂₃₃N₆₁O₃₁S₂ · xC₂HF₃O₂
• 分子量：: 3246.79 (free base basis)
• MDL號碼: MFCD18452843
• 分類程式碼代碼: 12352200
• PubChem物質ID: 329799971
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: lyophilized
• 顏色: white
• 溶解度: H₂O: >1 mg/mL
• 儲存溫度: −20°C
• SMILES 字串: 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 密鑰: MDUBLMWNQKKWEW-VECPGXDMSA-N

描述

一般說明

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).

應用

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.

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.

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.

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable