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555460-M

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Rhosin

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

Synonym(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

Empirical Formula (Hill Notation):
C20H18N6O
CAS Number:
1173671-63-0
Molecular Weight:
358.40
UNSPSC Code:
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.

Quality Level

100

Assay

≥93% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange-brown

solubility

DMSO: 10 mg/mL

storage temp.

2-8°C

General description

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.

Biochem/physiol Actions

Primary Target
Rho GTPase
Target Ki: 354 nM for RhoA

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases
Shang X, et al.
Chemistry and Biology, 19(6), 699-710 (2012)
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)
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)
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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