GGTI298

Cat. No.: HY-100876: Ficha de datos
SDS
Instrucciones de manejo
FAQs
Technical Support

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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 180977-44-0

Tamaño		Stock
MOQ		Minimum order quantity
50 mg		Obtener un presupuesto
100 mg		Obtener un presupuesto
250 mg		Obtener un presupuesto
Other size		Obtener un presupuesto

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of GGTI298:

GGTI298 Trifluoroacetate

Other Forms of GGTI298:

GGTI298 Trifluoroacetate In-stock

7 Publications Citing Use of MCE GGTI298

•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.

Recomendaciones destacadas

•Related Small Molecules:

•Related Proteins:

Actividad biológica
Protocolo
Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

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]

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].

MedChemExpress (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^[1].

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

Peso molecular

479.63

Fòrmula

C₂₇H₃₃N₃O₃S

No. CAS

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Pureza y Documentación

Ficha de datos (277 KB) SDS (252 KB) Instrucciones de manejo (2659 KB)

Referencias

[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]

Ensayo de quinasas ^[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. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Ensayo celular ^[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. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales ^[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. MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias	[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

Calculadora de molaridad
Calculadora de dilución

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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

Productos vistos recientemente:

Nombre del producto

Requested Quantity *

Nombre del solicitante *

Saludo

Direcciòn del E-mail *

Número de teléfono *

Department

Nombre de la Organizaciòn *

City

Provincia

Country or Region *

Observaciones

Nombre del producto

Lot #

Nombre del solicitante *

Direcciòn del E-mail *

Número de teléfono

Department *

Nombre de la Organizaciòn *

Country or Region *

Observaciones

Name
E-mail *

	Sorry, but the email address you supplied was invalid.

GGTI298

Other Forms of GGTI298:

GGTI298 Related Antibodies

7 Publications Citing Use of MCE GGTI298

Recomendaciones destacadas

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Protocolo

Pureza y Documentación

Referencias

Revisión del cliente

GGTI298 Related Antibodies

GGTI298 Related Classifications

Calculadora de molaridad

Calculadora de dilución