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Merck
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Principaux documents

555460-M

Millipore

Rhosin

≥93% (HPLC), powder, Rho inhibitor, Calbiochem®

Synonyme(s) :

Rho Inhibitor, Rhosin, G04, (2 R)-2-Amino-3-(1H-indol-3-yl)-Nʹ-((1 E)-quinoxalin-6-ylmethylidene)propanehydrazide, G04, (2R)-2-Amino-3-(1H-indol-3-yl)-Nʹ-((1E)-quinoxalin-6-ylmethylidene)propanehydrazide

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About This Item

Formule empirique (notation de Hill):
C20H18N6O
Numéro CAS:
1173671-63-0
Poids moléculaire :
358.40
Numéro MDL:
MFCD00005872
Code UNSPSC :
12352200

product name

Rho Inhibitor, Rhosin, Rho Inhibitor, Rhosin, CAS 1173671-63-0, is a cell-permeable compound that directly targets Rho GEF binding domain (Kd = 354 nM for RhoA), thereby prevents Rho from interacting with its GEFs.

Niveau de qualité

100

Pureté

≥93% (HPLC)

Forme

powder

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

orange-brown

Solubilité

DMSO: 10 mg/mL

Température de stockage

2-8°C

Description générale

Rhosin is composed of two aromatic rings connected by a linker and binds to the area surrounding Trp58 of RhoA with a Kd in the submicromolar range, effectively inhibiting GEF-catalyzed RhoA activation. This compound is valuable for studying the physiological role of RhoA subfamily GTPases and assessing the therapeutic potential of targeting Rho in pathological conditions.
Moreover, Rhosin can inhibit YAP activation by targeting RhoA and RhoC. It can also suppress tumor cell metastasis by inhibiting the Rho/YAP pathway and modulating the expression of RHAMM and CXCR4 in melanoma and breast cancer cells. It promotes stress resilience by enhancing D1-MSN plasticity and reducing hyperexcitability.

Application

Rho Inhibitor, Rhosin has been used to treat single breast tumor cells to regulate RhoA activity to validate the cell line with the Förster resonance energy transfer (FRET) biosensor.

Actions biochimiques/physiologiques

Primary Target
Rho GTPase
Target Ki: 354 nM for RhoA

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Shang, X., et al. 2012. Chem. Biol.19, 699.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Spatial and temporal dynamics of RhoA activities of single breast tumor cells in a 3D environment revealed by a machine learning-assisted FRET technique
Cheung BCH, et al.
Experimental Cell Research, 410(2), 112939-112939 (2022)
Rhosin suppressed tumor cell metastasis through inhibition of Rho/YAP pathway and expression of RHAMM and CXCR4 in melanoma and breast cancer cells
Tsubaki M, et al.
Biomedicines, 9(1), 35-35 (2021)
Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases
Shang X, et al.
Chemistry and Biology, 19(6), 699-710 (2012)
The selective RhoA inhibitor rhosin promotes stress resiliency through enhancing D1-medium spiny neuron plasticity and reducing hyperexcitability
Francis TC, et al.
Biological Psychiatry (2019)

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