规格

价格

库存

数量

25 mg

¥ 12,800

10-14周

50 mg

¥ 16,800

10-14周

100 mg

¥ 21,500

10-14周

生物活性

产品描述	GGTI298, a CAAZ peptidomimetic and potent geranylgeranyltransferase I (GGTase I) inhibitor, efficiently blocks the processing of geranylgeranylated Rap1A while exerting minimal impact on the processing of farnesylated Ha-Ras. The inhibitor displays in vivo IC50 values of 3 μM for Rap1A and >20 μM for Ha-Ras, respectively.
靶点活性	Ha-Ras:> 20 μM , Rap1A:3 μM
体外活性	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.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.
体内活性	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.

化学信息

分子量	479.63
分子式	C₂₇H₃₃N₃O₃S
CAS No.	180977-44-0
Smiles	C(N[C@H](C(OC)=O)CC(C)C)(=O)C1=C(C=C(NC[C@H](CS)N)C=C1)C=2C3=C(C=CC2)C=CC=C3
密度	1.190 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 100 mg/mL (208.49 mM), Sonication is recommended.

溶液配制表

DMSO

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

GGTI298