CAS NO: | 180977-44-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
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, withIC50values of 3 and >20 μM in vivo, respectively. | ||||||||||||||||
IC50& Target | IC50: 3 μM (Rap1A, in vivo), >20 μM (Ha-Ras, in vivo)[3] | ||||||||||||||||
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[1]. 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[2]. | ||||||||||||||||
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[1]. | ||||||||||||||||
分子量 | 479.63 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C27H33N3O3S | ||||||||||||||||
CAS 号 | 180977-44-0 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(208.49 mM;Need ultrasonic) 配制储备液
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