Reactivos e instrumentos para inmunología, biología celular y biología molecular.
 
> Belumosudil [911417-87-3]

Belumosudil [911417-87-3]

Imprimir Imprimir
Por favor conéctese

Referencia 10-4165-25mg

embalaje : 25mg

Marca : Focus Biomolecules

Solicitar más información

Contact local distributor :


Teléfono : +1 850 650 7790

Belumosudil | ROCK2 Inhibitor

CAS:
911417-87-3
Catalog Number:
10-4165
Activity:
Selective Rho kinase 2 (ROCK2) inhibitor
Chemical Names:
2-[3-[4-(1H-Indazol-5-yl)amino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide; KD025; SLx-2119
Molecular Weight:
452.52
Molecular Formula:
C26H24N6O2
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
White solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20 year as supplied from date of purchase. Solutions in DMSO may be stored at -20 month.
Shipping Code:
RT

Available Options

Size: Quantity 
5 mg$45.00
25 mg$145.00
Request Quote / Bulk / Custom Size
Product Inquiry

Belumosudil (911417-87-3) is a selective inhibitor of Rho kinase 2 (ROCK2) = 105 nM, ROCK1 = 24 It downregulated the ability of T cells to secrete IL-21 and IL-17, but not IFN-g, in response to T cell stimulation in vitro via a STAT3-dependent mechanism.2 Belumosudil ameliorated graft-versus-host disease in multiple models3,4 and was recently approved by the FDA for the treatment of GVHD (July 2021). It has also been shown to suppress adipogenesis.5-7 Suppression of adipocyte differentiation is mediated via casein kinase 2 inhibition (IC50 = 50 nM) and not ROCK2 inhibition.8

References:

  1. Boerma et al. (2008) Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin; Blood Coagul. Fibrinolysis. 709
  2. Zanin-Zhorov et al. (2014) Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism; Natl. Acad. Sci. USA 16814
  3. Flynn et al. (2016) Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism; 127 2144
  4. Jagasia et al. (2021) ROCK2 Inhibition with Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease; Clin. Invest. 1888
  5. Diep et al. (2018) Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells; Rep. 2477
  6. Diep et al. (2019) KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells; Adipocyte 114
  7. Wei et al. (2020) ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice; FASEB J. 474
  8. Tran and Chun (2021) ROCK2-Specific Inhibitor KD025 Suppresses Adipocyte Differentiation by Inhibiting Casein Kinase 2; Moleculespx;">26 4747
CAS:
911417-87-3
Catalog Number:
10-4165
Activity:
Selective Rho kinase 2 (ROCK2) inhibitor
Chemical Names:
2-[3-[4-(1H-Indazol-5-yl)amino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide; KD025; SLx-2119
Molecular Weight:
452.52
Molecular Formula:
C26H24N6O2
Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
White solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20 year as supplied from date of purchase. Solutions in DMSO may be stored at -20 month.
Shipping Code:
RT

Safety Data Sheet:

Download Safety Data Sheet

Product Data Sheet:

Download Product Data Sheet

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a restocking/refund fee

Belumosudil (911417-87-3) is a selective inhibitor of Rho kinase 2 (ROCK2) = 105 nM, ROCK1 = 24 It downregulated the ability of T cells to secrete IL-21 and IL-17, but not IFN-g, in response to T cell stimulation in vitro via a STAT3-dependent mechanism.2 Belumosudil ameliorated graft-versus-host disease in multiple models3,4 and was recently approved by the FDA for the treatment of GVHD (July 2021). It has also been shown to suppress adipogenesis.5-7 Suppression of adipocyte differentiation is mediated via casein kinase 2 inhibition (IC50 = 50 nM) and not ROCK2 inhibition.8

References:

  1. Boerma et al. (2008) Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin; Blood Coagul. Fibrinolysis. 709
  2. Zanin-Zhorov et al. (2014) Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism; Natl. Acad. Sci. USA 16814
  3. Flynn et al. (2016) Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism; 127 2144
  4. Jagasia et al. (2021) ROCK2 Inhibition with Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease; Clin. Invest. 1888
  5. Diep et al. (2018) Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells; Rep. 2477
  6. Diep et al. (2019) KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells; Adipocyte 114
  7. Wei et al. (2020) ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice; FASEB J. 474
  8. Tran and Chun (2021) ROCK2-Specific Inhibitor KD025 Suppresses Adipocyte Differentiation by Inhibiting Casein Kinase 2; Moleculespx;">26 4747