NE 10790

SKU: orb1307972

Description

NE 10790

Research Area

Metabolism Research

Images & Validation

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Key Properties

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CAS Number	152831-36-2
MW	247.14
Purity	100.00%
Formula	C₈H₁₀NO₆P
SMILES	C(CC=1C=CC=NC1)(P(=O)(O)O)(C(O)=O)O
Target	Others,Transferase
Solubility	H2O:1 mg/mL (4.05 mM);DMSO:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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In Vitro

NE 10790 did inhibit prenylation in J774 macrophages and osteoclasts, but only of proteins of molecular mass approximately 22-26 kDa, the prenylation of which was not affected by peptidomimetic inhibitors of either farnesyl transferase (FTI-277) or geranylgeranyl transferase I (GGTI-298). These 22-26-kDa proteins were shown to be geranylgeranylated by labelling J774 cells with [(3)H]geranylgeraniol. Furthermore, NE10790 inhibited incorporation of [(14)C]mevalonic acid into Rab6, but not into H-Ras or Rap1, proteins that are modified by FTase and GGTase I, respectively. These data demonstrate that NE10790 selectively prevents Rab prenylation in intact cells. In accord, NE10790 inhibited the activity of recombinant Rab GGTase in vitro, but did not affect the activity of recombinant FTase or GGTase I. NE10790 therefore appears to be the first specific inhibitor of Rab GGTase to be identified. In contrast to risedronate, NE10790 inhibited bone resorption in vitro without markedly affecting osteoclast number or the F-actin 'ring' structure in polarized osteoclasts. However, NE10790 did alter osteoclast morphology, causing the formation of large intracellular vacuoles and protrusion of the basolateral membrane into large, 'domed' structures that lacked microvilli. The anti-resorptive activity of NE10790 is thus likely due to disruption of Rab-dependent intracellular membrane trafficking in osteoclasts.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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3-PEHPC, inhibit, NE 10790, NE10790, NE-10790, FPP synthase, FPPS, Inhibitor

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Compound Identifiers

PubChem CID

10014835 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	152831-36-2
MW:	247.14
Formula:	C₈H₁₀NO₆P

NE 10790

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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