GLPBio

GGTI298

Catalog No.: GC36134Purity:>99.50%
COASDSData Sheet
GGTI298 is a selective, irreversible inhibitor of geranylgeranyltransferase I (GGTase-I) (IC50 = 3μM).

Products are for research use only. Not for human use. We do not sell to patients.

GGTI298
Cas No.: 180977-44-0
10mM (in 1mL DMSO)In Stock
$176.00
1
1mgIn Stock
$83.00
1
5mgIn Stock
$167.00
1
10mgIn Stock
$260.00
1
25mgIn Stock
$510.00
1
50mgIn Stock
$695.00
1
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Description

GGTI298 is a selective, irreversible inhibitor of geranylgeranyl transferase I (GGTase-I) (IC50 = 3μM) [1]. By inhibiting GGTase-I, GGTI298 blocks geranylgeranylation of small GTPases such as RhoA, leading to cell cycle arrest at the G0/G1 phase and induction of apoptosis [2-3]. GGTI298 is primarily used to treat non-small cell lung cancer [4].

In A549 cells, Gefitinib and GGTI298 (2.5-5µM; 48h) have synergistic anti-proliferative effects on cells [5]. In A549 cells, GGTI298 (15µM; 48h) induces cell apoptosis [6].

In Luc-G33 cells xenograft mice model, combination treatment with Zoledronate and GGTI298 (1.16mg/kg; sc; 35d) both reduced tumor growth [7].

References:
[1]. Dan H C, Jiang K, Coppola D, et al. GGTI 298[J]. Oncogene, 2004, 23: 706-715.
[2]. Peterson Y K, Kelly P, Weinbaum C A, et al. A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity[J]. Journal of Biological Chemistry, 2006, 281(18): 12445-12450.
[3]. Vogt A, Sun J, Qian Y, et al. The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21WAF1/CIP1/SDI1 in a p53-independent manner[J]. Journal of Biological Chemistry, 1997, 272(43): 27224-27229.
[4]. Chen S, Fu L, Raja S M, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis[J]. Molecular cancer, 2010, 9(1): 23.
[5]. Liu B S, Dai X Y, Xia H W, et al. Geranylgeranyl transferase 1 inhibitor GGTI-298 enhances the anticancer effect of gefitinib[J]. Molecular Medicine Reports, 2018, 18(4): 4023-4029.
[6]. Miquel K, Pradines A, Sun J, et al. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells[J]. Cancer research, 1997, 57(10): 1846-1850.
[7]. Lau C P Y, Wong K C, Huang L, et al. A mouse model of luciferase-transfected stromal cells of giant cell tumor of bone[J]. Connective tissue research, 2015, 56(6): 493-503.

Protocol

Cell experiment [1]:

Cell lines

A549 cells

Preparation Method

A549 cells were seeded (5×103 cells per well in 100µL DMEM with 10% FBS) in a 96-well flat-bottomed plate at 24h prior to treatment. A549 cells were treated with gefitinib (5µM) and/or GGTI298 (concentration indicated) for 48h at 37℃ in a humidified (5% CO2, 95% air) incubator. Following incubation at 37℃, cell growth was measured using a Cell Counting Kit-8.

Reaction Conditions

2.5-5µM; 48h

Applications

Gefitinib and GGTI298 have synergistic anti-proliferative effects on cells.
Animal experiment [2]:

Animal models

Luc-G33 cells xenograft mice model

Preparation Method

The nude mice were initially weighed and anesthetized intraperitoneally with 10% chloral hydrate at 0.1ml/30g live weight. The operative area was prepared with iodine. Each mouse was then given an intraosseous (1×106) and a subcutaneous injection (3×106) of Luc-G33 cells in hydrogel into the tibia and under the dorsal skin, respectively. A preliminary study had been proceeded on eight mice for observing the duration of the BLI signals from the Luc-G33 cells in the mice in vivo. Thirty-two mice after Luc-G33 implantation were randomly divided into four groups (8 mice/group) with equal average body weight and drugs were given to each mice three days after cell injection. Group 1 was then given 0.9% sodium chloride (Abbott) as the vehicle control treatment; Groups 2–4 were given Zoledronate (ZOL) and GGTI298 treatments at the following dosages: group 2 treated with ZOL alone at 400mg/kg; group 3 with GGTI298 alone at 1.16mg/kg; and group 4 with the combination of ZOL at 400mg/kg and GGTI298 at 1.16mg/kg.

Dosage form

1.16mg/kg; sc; 35d

Applications

Combination treatment with Zoledronate and GGTI298 both reduced tumor proliferation.

References:
[1]. Liu B S, Dai X Y, Xia H W, et al. Geranylgeranyl transferase 1 inhibitor GGTI-298 enhances the anticancer effect of gefitinib[J]. Molecular Medicine Reports, 2018, 18(4): 4023-4029.
[2]. Lau C P Y, Wong K C, Huang L, et al. A mouse model of luciferase-transfected stromal cells of giant cell tumor of bone[J]. Connective tissue research, 2015, 56(6): 493-503.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
180977-44-0
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
Molecular Formula
C27H33N3O3S
Molecular Weight
479.63
Solubility
DMSO: 100 mg/mL (208.49 mM); Water: < 0.1 mg/mL (insoluble)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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