GGTI298

製品番号: HY-100876: Data Sheet 取扱説明書
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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 IC₅₀ values of 3 and > 20 μM in vivo, respectively.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (GGTI298 Trifluoroacetate) that retains the same biological activity.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 180977-44-0

容量		在庫状況
MOQ		Minimum order quantity
50 mg		お問い合わせ
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This product is a controlled substance and not for sale in your territory.

Other 在庫あり Forms of GGTI298:

GGTI298 Trifluoroacetate

Other Forms of GGTI298:

GGTI298 Trifluoroacetate 在庫あり

顧客検証

•J Oral Biosci. 2023 Dec;65(4):347-355. [Abstract]

Cell Imaging/Staining

In Vivo Efficacy Study

Histological Imaging/Staining

: GGTI298 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]; SH-SY5Y cells were transfected with Flag-GBP2, Flag-GBP2-ΔCAAX, or treated with the geranylgeranylation inhibitor GGTI298 Trifluoroacetate (10 μM) for 48 h.

: GGTI298 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]; SH-SY5Y cells were transfected with Flag-GBP2, Flag-GBP2-ΔCAAX, or treated with the geranylgeranylation inhibitor GGTI298 Trifluoroacetate (10 μM) for 48 h.

: GGTI298 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]; Co-IP assays in HEK293T cells show that GGTI298 Trifluoroacetate treatment or expression of the GBP2-ΔCAAX mutant impairs the interaction between GBP2 and NIX.

: GGTI298 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]; Behavioral tests (open field, pole, rotarod) demonstrate that GGTI298 Trifluoroacetate (12 mg/kg daily for fourteen consecutive days, ip) treatment ameliorates MPTP-induced motor deficits.

: GGTI298 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104029. [Abstract]; IHC for TH in the substantia nigra and striatum show that GGTI298 Trifluoroacetate (12 mg/kg daily for fourteen consecutive days, ip) treatment preserves dopaminergic neurons.

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生物活性
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純度とドキュメンテーション
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製品説明

IC₅₀ & Target

IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	30 μM Compound: GGTI-298	Antimalarial activity against Plasmodium berghei NK65 infected in human HepG2 cells after 48 hrs by RT-PCR Antimalarial activity against Plasmodium berghei NK65 infected in human HepG2 cells after 48 hrs by RT-PCR	[PMID: 20457823]

体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

479.63

分子式

C₂₇H₃₃N₃O₃S

CAS 番号

180977-44-0

Appearance

Solid

Color

White to gray

SMILES

CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

純度とドキュメンテーション

取扱説明書 (2659 KB)

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 [Content Brief]

[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. [Content Brief]

[3]. McGuire TF, et al. Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation. J Biol Chem. 1996 Nov 1;271(44):27402-7. [Content Brief]

キナーゼ実験 ^[2]	The given cells are lysed with Reporter Lysis Buffer and subjected to luciferase activity assay using Luciferase Assay System in a luminometer. Relative luciferase activity is normalized to protein content. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
細胞実験 ^[2]	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. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	The ileal loop experiment is performed in 6-8-week-old mice by a modified rabbit ileal loop assay. Following gut sterilization, the animals are kept fasted for 24 h prior to surgery and fed only water ad libitum. Anesthesia is induced by a mixture of ketamine (35 mg/kg of body weight) and xylazine (5 mg/kg of body weight). A laparotomy is performed, and the experimental loops of 5-cm length are constricted at the terminal ileum by tying with non-absorbable silk. The following fluids are instilled in each loop by means of a tuberculin syringe fitted with a disposable needle through the ligated end of the loop as the ligatured is tightened: pure CT (1 μg; positive control), saline (negative control), CT (1 μg) + TRAM-34 (different concentrations in μM as indicated in Fig. 7), CT (1 μg) + H1152 (1 μM), and CT (1 μg) + GGTI298 (different concentrations in μM), a specific inhibitor of Rap1A. The intestine is returned to the peritoneum, and the mice are sutured and returned to their cages. After 6 h, these animals are sacrificed by cervical dislocation, and the loops are excised. The fluid from each loop is collected, and the ratio of the amount of fluid contained in the loop with respect to the length of the loop (fluid accumulation ratio in g/cm) is calculated as a reflection of the efficacy of various inhibitors. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
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 [Content Brief] [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. [Content Brief] [3]. McGuire TF, et al. Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation. J Biol Chem. 1996 Nov 1;271(44):27402-7. [Content Brief]

GGTI298 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GGTI298180977-44-0GGTI 298GGTI-298ApoptosisInhibitorinhibitorinhibit

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