Belumosudil, ROCK2 inhibitor (TBI4165)
$81.00 – $261.00
ROCK2 inhibitor
SKU | Stock | SIZE (mg) | Price | Quantity | ||
---|---|---|---|---|---|---|
TBI4165-5MG | Yes | 5 MG | $81.00 | |||
TBI4165-25MG | Yes | 25 MG | $261.00 |
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Description
Product Details
Formal Name: 2-[3-[4-(1H-Indazol-5-yl)amino)quinazolin-2-yl]phenoxy]-N-propan-2-ylacetamide
Alternate Names: KD025; SLx-2119
Molecular Formula: C26H24N6O2
Formula Weight: 452.50
CAS Number: 911417-87-3
Purity: >98%
Formulation: powder
Solubility: Soluble in DMSO (up to 25 mg/ml)
Storage: -20°C
Stability: ≥ 1 year.
Applications
ROCK2 inhibitor
Functions
Belumosudil is a selective inhibitor of Rho kinase 2 (ROCK2) – IC50’s: ROCK2 = 105 nM, ROCK1 = 24 µM in enzyme assays. It downregulated the ability of T cells to secrete IL-21 and IL-17, but not IFN-γ, in response to T cell stimulation in vitro via a STAT3-dependent mechanism. Belumosudil ameliorated graft-versus-host disease in multiple models and was recently approved by the FDA for the treatment of GVHD (July 2021). It has also been shown to suppress adipogenesis. Suppression of adipocyte differentiation is mediated via casein kinase 2 inhibition (IC50 = 50 nM) and not ROCK2 inhibition.
Application Procedures
First dissolved in DMSO (up to 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.
Additional information
SIZE (mg) | 25 MG, 5 MG |
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