Y16 - 10mM in DMSO, high purity , CAS No.429653-73-6

  • 10mM in DMSO
Item Number
Y423943
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Y423943-1ml
1ml
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Rho Inhibitors

Basic Description

Synonyms429653-73-6 | Y16 | CHEMBL485210 | (E)-4-(3-((3-methylbenzyl)oxy)benzylidene)-1-phenylpyrazolidine-3,5-dione | (4E)-4-[[3-[(3-methylphenyl)methoxy]phenyl]methylidene]-1-phenylpyrazolidine-3,5-dione | BDBM50274241 | s6752 | STL368063 | AKOS005166252 | AKOS005166258 | CS-3879 |
Specifications & Purity10mM in DMSO
Biochemical and Physiological MechanismsY16 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).
Storage TempStore at -80°C
Shipped InIce chest + Ice pads
Product Description

Information

Y16 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).

Targets

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, Y16 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, Y16 inhibits mammary sphere formation of MCF7 breast cancer cells but does not affect the nontransforming MCF10A cells. Y16 works synergistically with Rhosin/G04, a Rho GTPase activation site inhibitor, in inhibiting LARG–RhoA interaction, RhoA activation, and RhoA-mediated signaling functions. Y16 effectively inhibits the growth, migration, and invasion activities of breast cancer cells.

Cell Research(from reference)

Cell lines:PC-3 cells 

Concentrations:10 μM 

Incubation Time:36 h 

Associated Targets(Human)

ARHGEF12 Tchem Rho guanine nucleotide exchange factor 12 (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ROCK2 Tclin Rho-associated protein kinase 2 (6206 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR1H4 Tclin Bile acid receptor FXR (6228 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCF7 (126967 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio Transforming protein RhoA (190 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIO Tbio Triple functional domain protein (3 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ITSN1 Tbio Intersectin-1 (4 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ARHGEF12 Tchem Rho guanine nucleotide exchange factor 12 (11 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio Rho GEF 11/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio A-kinase anchor protein 13/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PKN1 Tchem Serine/threonine-protein kinase N1/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio RhoGEF 1/Transforming protein RhoA (12 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio Rho GTPase-activating protein 35/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio Protein diaphanous homolog 1/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RHOA Tbio Proto-oncogene DBL/Transforming protein RhoA (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NIH3T3 (5395 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (4E)-4-[[3-[(3-methylphenyl)methoxy]phenyl]methylidene]-1-phenylpyrazolidine-3,5-dione
INCHI InChI=1S/C24H20N2O3/c1-17-7-5-9-19(13-17)16-29-21-12-6-8-18(14-21)15-22-23(27)25-26(24(22)28)20-10-3-2-4-11-20/h2-15H,16H2,1H3,(H,25,27)/b22-15+
InChi Key ITMLWGWTDWJSRZ-PXLXIMEGSA-N
Canonical SMILES CC1=CC(=CC=C1)COC2=CC=CC(=C2)C=C3C(=O)NN(C3=O)C4=CC=CC=C4
Isomeric SMILES CC1=CC(=CC=C1)COC2=CC=CC(=C2)/C=C/3\C(=O)NN(C3=O)C4=CC=CC=C4
WGK Germany 3
PubChem CID 989521
Molecular Weight 384.43

Certificates

Certificate of Analysis(COA)

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Safety and Hazards(GHS)

WGK Germany 3
RIDADR UN30779/PGIII

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