1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. FAZ-3780

FAZ-3780 is an inhibitor that binds to the NTF2L domain of G3BP1/2. FAZ-3780 binds to the NTF2L nsP3 of G3BP1 with high affinity, with a Kd of 0.15 μM and a Pep-FRET IC50 of 0.7 μM. FAZ-3780 targets the protein-protein interaction domain of G3BP1/2, and specifically inhibits the co-condensation of G3BP1, caprin 1 and RNA in vitro. FAZ-3780 inhibits stress granule formation and disassembles pre-formed stress granules. FAZ-3780 can be used in studies related to cancer and neurodegenerative diseases.

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FAZ-3780

FAZ-3780 Chemical Structure

CAS No. : 3036029-78-1

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Based on 2 publication(s) in Google Scholar

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Description

FAZ-3780 is an inhibitor that binds to the NTF2L domain of G3BP1/2. FAZ-3780 binds to the NTF2L nsP3 of G3BP1 with high affinity, with a Kd of 0.15 μM and a Pep-FRET IC50 of 0.7 μM. FAZ-3780 targets the protein-protein interaction domain of G3BP1/2, and specifically inhibits the co-condensation of G3BP1, caprin 1 and RNA in vitro. FAZ-3780 inhibits stress granule formation and disassembles pre-formed stress granules. FAZ-3780 can be used in studies related to cancer and neurodegenerative diseases[1].

In Vitro

FAZ-3780 (G3Ib) (5-50 μM; 2 h) dose-dependently disrupts the interactions between G3BP1 and endogenous caprin 1 as well as USP10 in U2OS cell lysates[1].
FAZ-3780 (25-50 μM; 2 h) disrupts the interaction between the isolated NTF2L domain of G3BP1 and endogenous caprin 1 and USP10 in HEK293T cell lysates[1].
FAZ-3780 (0.001-100 μM; 70 min) potently inhibits the in vitro co-condensation of human G3BP1, caprin 1 and RNA, with an IC50 of 3.450 μM[1].
FAZ-3780 (5-50 μM; 50 min) inhibits sodium arsenite-induced stress granule formation in U2OS/HeLa G3BP1-GFP cells, rapidly disassembles stress granules, and prevents the localization of TDP-43 to stress granules[1].
FAZ-3780 (5-50 μM; 24 h) exhibits sustained and potent inhibitory activity against sodium arsenite-induced stress granule formation in U2OS cells[1].
FAZ-3780 (50 μM; 50 min) inhibits heat shock-induced stress granule formation in U2OS G3BP1-GFP cells and rapidly disassembles pre-formed heat shock-induced stress granules in cells[1].

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

Western Blot Analysis[1]

Cell Line: U2OS cells stably expressing G3BP1-GFP
Concentration: 5, 20, 50 μM
Incubation Time: 2 h
Result: Resulted in a dose-dependent reduction of
the interaction between G3BP1 and both endogenous caprin
1 and endogenous USP10.

Western Blot Analysis[1]

Cell Line: HEK293T cells expressing GFP-NTF2L
Concentration: 25, 50 μM
Incubation Time: 2 h
Result: Disrupted the interaction of the isolated NTF2L domain of G3BP1 with endogenous caprin 1 and USP10.

Immunofluorescence[1]

Cell Line: U2OS/Hela G3BP1-GFP cells
Concentration: 5, 20, 50 μM
Incubation Time: 50 min
Result: Inhibited sodium arsenite-induced G3BP1-GFP signal.
Inhibited heat shock-induced G3BP1-GFP signal.
Rapidly disassembled preformed sodium arsenite-induced G3BP1-GFP signal.
Rapidly disassembled preformed heat shock-induced G3BP1-GFP signal.
Molecular Weight

606.80

Formula

C35H50N4O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@H](C)C(N1CCC[C@@H]1C2=CC=CC=C2)=O)[C@@H](NC([C@H](C(C)(C)O)NC(CCC(C)(C)C)=O)=O)[C@@H](C)C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (82.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6480 mL 8.2399 mL 16.4799 mL
5 mM 0.3296 mL 1.6480 mL 3.2960 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.68%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6480 mL 8.2399 mL 16.4799 mL 41.1997 mL
5 mM 0.3296 mL 1.6480 mL 3.2960 mL 8.2399 mL
10 mM 0.1648 mL 0.8240 mL 1.6480 mL 4.1200 mL
15 mM 0.1099 mL 0.5493 mL 1.0987 mL 2.7466 mL
20 mM 0.0824 mL 0.4120 mL 0.8240 mL 2.0600 mL
25 mM 0.0659 mL 0.3296 mL 0.6592 mL 1.6480 mL
30 mM 0.0549 mL 0.2747 mL 0.5493 mL 1.3733 mL
40 mM 0.0412 mL 0.2060 mL 0.4120 mL 1.0300 mL
50 mM 0.0330 mL 0.1648 mL 0.3296 mL 0.8240 mL
60 mM 0.0275 mL 0.1373 mL 0.2747 mL 0.6867 mL
80 mM 0.0206 mL 0.1030 mL 0.2060 mL 0.5150 mL
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Product Name:
FAZ-3780
Cat. No.:
HY-162289
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