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GGTI 2133 TFA

CAT: 0931-T85180-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T85180-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
1217480-14-2
Target
Others, YAP
Related Pathways
Others, Stem Cells
Bioactivity
GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM) . The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 μM) without affecting the farnesylation of H-Ras (IC50= >30 μM) . Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg) .
Smiles
OC(=O)C(F)(F)F.CC(C)C[C@H](NC(=O)c1ccc(NCc2c[nH]cn2)cc1-c1cccc2ccccc12)C(O)=O
Molecular Formula
C29H29F3N4O5
Molecular Weight
570.569
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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