2. Apoptosis
  3. Apoptosis
  4. GGTI-2154

GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (GGTI-2154 hydrochloride) usually boasts enhanced water solubility and stability.

For research use only. We do not sell to patients.

GGTI-2154 Chemical Structure

GGTI-2154 Chemical Structure

CAS No. : 251577-10-3

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GGTI-2154 Related Antibodies

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Description

GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer[1][2].

IC50 & Target

IC50: 21 nM (GGTase I)[1]
In Vitro

GGTI-2154 inhibits the transfer of geranylgeranyl from [3H]GGPP to H-Ras CVLL, with an IC50 of 21 nM[1].

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

GGTI-2154 Related Antibodies
In Vivo

GGTI-2154 (100 mg/kg/day; s.c. for 14 days) induces breast tumor regression in MMTV-ν-Ha-Ras transgenic mice[2].
GGTI-2154 (50 mg/kg/day; i.p. for 50 day) inhibits A-549 tumor growth in nude mice by 60%[1].

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

Animal Model: MMTV-v-Ha-ras transgenic mice bearing mammary carcinoma[2]
Dosage: 100 mg/kg/day
Administration: S.c. with osmotic mini-pumps for 14 days
Result: Halted the tumors aggressive growth.
Resulted in rapid tumor regression within 3 days of initiation of drug treatment.
Molecular Weight

420.50

Formula

C24H28N4O3
CAS No.
SMILES

CC(C)C[C@@H](C(O)=O)NC(C1=CC=C(NCC2=CN=CN2)C=C1C3=CC=CC=C3C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GGTI-2154 Related Classifications

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× = ×
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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:

GGTI-2154251577-10-3GGTI2154GGTI 2154ApoptosisgeranylgeranyltransferaseIGGTasecancerInhibitorinhibitorinhibit

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