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SB-505124 hydrochloride

SKU: orb1705004

Description

SB-505124 hydrochloride is a potent, selective, and orally active inhibitor of TGF-β type I receptors (ALK4/5/7). It has been shown to inhibit IL-6 production in synovial explants and reduce Th17 differentiation in mice, making it a valuable tool for studying pathways in inflammation, autoimmunity, and cancer research such as colorectal cancer.

Research Area

Cardiovascular Research, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number356559-13-2
MW371.86
Purity98.71% (May vary between batches)
FormulaC20H22ClN3O2
SMILESCl.N=1C(=CC=CC1C)C=2N=C(NC2C=3C=CC=4OCOC4C3)C(C)(C)C
TargetALK,TGF-beta/Smad
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.38 mM);Methanol:120 mg/mL (322.7 mM);DMSO:40 mg/mL (107.57 mM)

Bioactivity

In Vivo
SB-505124 (5 mg/kg; i.p.) alone does not elicit any response in C57Bl6 mice bearing A549 xenografts. However, when combined with a single dose of Carboplatin (60 mg/kg), SB-505124 induces sustained therapeutic effects in five subjects, eliminating the need for ongoing maintenance therapy. This synergy presents a potent treatment strategy without continuous intervention in the specified animal model, highlighting its potential efficacy.
In Vitro
METHODS: Rabbit subconjunctival fibroblasts were incubated with 10 μM SB-505124 or 0.04% MMC and then incubated with or without TGF-β2 (2 ng/ml) in 12-well plates for 48 h. The effects of ALK-5 inhibitor SB-505124 on TGF-β2-induced downstream effects were analyzed by Western blotting. RESULTS: The levels of pSmad2, CTGF, and α-SMA in rabbit subconjunctival fibroblasts treated with SB-505124 were decreased in a concentration-dependent manner.

Storage & Handling

Storagekeep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SB 505124 hydrochloride, SB505124 hydrochloride, SB-505124 Hydrochloride, ALK4, ALK5, ALK7
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Key Properties

No computed properties available.

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Protocol Information

SB-505124 hydrochloride (orb1705004)

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% DMSO +
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% Tween 80 +
%

Available Sizes

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1 mg
$ 80.00
5 mg
$ 120.00
10 mg
$ 150.00
25 mg
$ 240.00
50 mg
$ 370.00
100 mg
$ 530.00
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