Home Cell Cycle Rho inhibitor Y16

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Y16 Rho inhibitor

Cat.No.S6752

Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM).
Y16 Rho inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 384.43

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Quality Control

Batch: S675201 DMSO]39 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.24%
99.24

Solubility

In vitro
Batch:

DMSO : 39 mg/mL (101.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 384.43 Formula

C24H20N2O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 429653-73-6 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=CC=C1)COC2=CC=CC(=C2)C=C3C(=O)NN(C3=O)C4=CC=CC=C4

Mechanism of Action

Targets/IC50/Ki
RhoGEFs
In vitro

Y16 binds to the junction site of the DH-PH domains of LARG with a ∼80 nM Kd and suppresses LARG catalyzed RhoA activation dose dependently. It is active in blocking the interaction of LARG and related G-protein–coupled Rho GEFs with RhoA without a detectable effect on other DBL family Rho GEFs, Rho effectors, or a RhoGAP. In cells, this compound selectively inhibits serum-induced RhoA activity and RhoA-mediated signaling, effects that can be rescued by a constitutively active RhoA or ROCK mutant. By suppressing RhoA activity, it inhibits mammary sphere formation of MCF7 breast cancer cells but does not affect the nontransforming MCF10A cells. This chemical works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG–RhoA interaction, RhoA activation, and RhoA-mediated signaling functions. It effectively inhibits the growth, migration, and invasion activities of breast cancer cells.
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