Belumosudil | ROCK2 Inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $45.00 | ||
| 25 mg | $145.00 |
Belumosudil (911417-87-3) is a selective inhibitor of Rho kinase 2 (ROCK2) – IC50’s: ROCK2 = 105 nM, ROCK1 = 24 µM in enzyme assays.1 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:
- 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. 19 709
- 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 111 16814
- Flynn et al. (2016) Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism; 127 2144
- Jagasia et al. (2021) ROCK2 Inhibition with Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease; Clin. Invest. 39 1888
- Diep et al. (2018) Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells; Rep. 8 2477
- Diep et al. (2019) KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells; Adipocyte 9 114
- Wei et al. (2020) ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice; FASEB J. 34 474
- Tran and Chun (2021) ROCK2-Specific Inhibitor KD025 Suppresses Adipocyte Differentiation by Inhibiting Casein Kinase 2; Molecules 26 4747
NMR (Conforms)
Safety Data Sheet:
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 $20 restocking/refund fee
Belumosudil (911417-87-3) is a selective inhibitor of Rho kinase 2 (ROCK2) – IC50’s: ROCK2 = 105 nM, ROCK1 = 24 µM in enzyme assays.1 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:
- 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. 19 709
- 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 111 16814
- Flynn et al. (2016) Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism; 127 2144
- Jagasia et al. (2021) ROCK2 Inhibition with Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease; Clin. Invest. 39 1888
- Diep et al. (2018) Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells; Rep. 8 2477
- Diep et al. (2019) KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells; Adipocyte 9 114
- Wei et al. (2020) ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice; FASEB J. 34 474
- Tran and Chun (2021) ROCK2-Specific Inhibitor KD025 Suppresses Adipocyte Differentiation by Inhibiting Casein Kinase 2; Molecules 26 4747
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