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Product details

名称

GGTI298

分子类型

小分子

英文名称

GGTI298

货号

G649880-5mg

包装规格

5mg

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Assay Cells are seeded in 96-well cell culture plates and treated the next day with the agents indicated. The viable cell number is determined using the sulforhodamine B assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)

生化机理

GGTI298 是一种 CAAZ 多肽仿麦角酰基转移酶 I (GGTase I) 抑制剂，它能强烈抑制麦角酰基化 Rap1A 的处理，而对法尼基化 Ha-Ras 的处理影响很小。

CAS号

180977-44-0

分子式

C27H33N3O3S

分子量

479.63 g/mol

PubChem编号

9811606

Isomeric SMILES

CC(C)C[C@@H](C(=O)OC)NC(=O)C1=C(C=C(C=C1)NC[C@H](CS)N)C2=CC=CC3=CC=CC=C32

Smiles

CC(C)C[C@@H](C(=O)OC)NC(=O)C1=C(C=C(C=C1)NC[C@H](CS)N)C2=CC=CC3=CC=CC=C32

PubChem CID

9811606

溶解性

DMSO : 100 mg/mL (208.49 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

479.224 Da

单同位素质量Monoisotopic Mass

479.224 Da

拓扑极表面积Topological Polar Surface Area

94.500 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

661.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

5.100

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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