GGTI298|180977-44-0|-陌孚医药/Medlife

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GGTI298

目录号: PL10886

CAS No. :180977-44-0

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中文名称	GGTI298
中文别名	GGTI-298
英文名称	GGTI298
英文别名	L-Leucine,N-[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-, methylester;GGTI 298;GGTI-298;methyl (2S)-2-[[4-[[(2R)-2-amino-3-sulfanylpropyl]amino]-2-naphthalen-1-ylbenzoyl]amino]-4-methylpentanoate,2,2,2-trifluoroacetic acid;L-Leucine,N-[4-[(2-amino-3-mercaptopropyl)amino]-2-(1-naphthalenyl)benzoyl]-, methylester, (R)-;N-[4-[2(R)-AMino-3-Mercaptopropyl]aMino-2-(1-naphthalenyl)benzoyl]-L-leucineMethylestertrifluoroacetatesalt;GGTI298 (CF3CO2H)salt;GGTI-298 trifluoroacetate salt;N-4-[2(R)-AMINO-3-MERCAPTOPROPYL]AMINO-2-NAPHTHYLBENZOYL-(L)-LEUCINE METHYL ESTER, TFA;N-[[4-(2-(R)-AMINO-3-MERCAPTOPROPYL)AMINO]-2-NAPHTHYLBENZOYL]LEUCINE METHYL ESTER TRIFLUOROACETATE SALT;N-[[4-(2-(R)-Amino-3-mercaptopropyl)amino]-2-naphthylbenzoyl]leucine methyl ester trifluoroacetate salt;GGTI298 Trifluoroacetate;GGTI298 (Trifluoroacetate);GGTI 298 TFA salt;GGTI 298 trifluoroacetate salt hydrate;AOB33796;BCP24853;s7466;GGTI298 trifluoroacetate salt hydrate;GGTI 298 trifluoroacetate salt hydrate, >=90% (HPLC), film;(S)-methyl 2-(4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methyl;GGTI298
Cas No.	180977-44-0
分子式	C₂₉H₃₄F₃N₃O₅S
分子量	593.66
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	GGTI298 是有效的 GGTase I 抑制剂，能够抑制 geranylgeranylated Rap1A 的过程，对 farnesylated Ha-Ras 的过程也有一定影响，在体内，IC₅₀ 值分别为 3 和 > 20 μM。
生物活性	GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC 50 values of 3 and > 20 μM in vivo, respectively.
性状	Solid
IC50 & Target[1][2]	IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)
体外研究(In Vitro)	Both RhoA inhibitor (GGTI298) and ROCK inhibitor (H1152) significantly reduce cAMP agonist-stimulated IK(ap), whereas the latter additionally reduces colocalization of KCNN4c with the apical membrane marker wheat germ agglutinin in T84WT cells. Knockdown of DR4 abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis induced by the combination of GGTI298 and TRAIL. GGTI298/TRAIL activates NF-κB and inhibits Akt. knockdown of DR5, preventes GGTI298/TRAIL-induced IκBα and p-Akt reduction, suggesting that DR5 mediates reduction of IκBα and p-Akt induced by GGTI298/TRAIL. In contrast, DR4 knockdown further facilitates GGTI298/TRAIL-induced p-Akt reduction. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Sheikh IA, et al. The Epac1 signaling pathway regulates Cl- secretion via modulation of apical KCNN4c channels in diarrhea. J Biol Chem. 2013 Jul 12;288(28):20404-15 [2]. Chen S, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis. Mol Cancer. 2010 Jan 29;9:23.

溶解度数据	In Vitro: DMSO : 100 mg/mL (208.49 mM; Need ultrasonic)配制储备液

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