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BMS-509744

SKU: orb1707536

Description

BMS-509744 is a potent and selective ATP-competitive inhibitor of interleukin-2-inducible T-cell kinase (Itk), exhibiting an IC50 of 19 nM. It has demonstrated efficacy in reducing IL-8 expression and HIV infection in vitro, as well as ameliorating pulmonary inflammation in allergic asthma and Imiquimod-induced skin inflammation in murine models.

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Protein Biochemistry, Signal Transduction

Images & Validation

Key Properties

CAS Number439575-02-7
MW623.83
Purity99.70% (May vary between batches)
FormulaC32H41N5O4S2
SMILESO=C(NC1=NC=C(S1)SC2=CC(=C(OC)C=C2C)C(=O)N3CCN(C(=O)C)CC3)C4=CC=C(C=C4)CNC(C)C(C)(C)C
TargetHIV Protease,Immunology/Inflammation related,Tyrosine Kinases,IL Receptor,Others
Solubility10% DMSO+40% PEG300+5% Tween-80+45% Saline:2.5 mg/mL (4.01 mM);DMSO:52 mg/mL (83.36 mM)

Bioactivity

Target IC50
ITK:19 nM
In Vivo
BMS-509744 (10 mg/kg, intraperitoneal injection, once daily for 10 consecutive days) alleviated sepsis-associated depressive-like behaviors in a mouse model of sepsis by inhibiting ITK signaling, modulating the Th17/Treg balance, reducing IL-17A-mediated neuroinflammation and oxidative stress, and activating the Nrf2 antioxidant pathway .
In Vitro
BMS-509744 (2μM, 24 hours) specifically inhibits ITK phosphorylation and downstream PLCγ1 activity (without affecting the MEK/AKT pathway) in Parazacco spilurus subsp. spilurus, significantly reducing T-cell calcium flux response, IL-2/IL-21 secretion, and CXCL12-induced migration capacity. Moreover, it exhibits synergistic antitumor effects when combined with doxorubicin or PI3K inhibitors .

Storage & Handling

Storagestore at low temperature | 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

BMS 509744, BMS509744, BMS-509744, Itk

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Key Properties

No computed properties available.

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BMS-509744 (orb1707536)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 80.00
2 mg
$ 100.00
5 mg
$ 140.00
1 ml x 10 mM (in DMSO)
$ 170.00
10 mg
$ 210.00
25 mg
$ 420.00
50 mg
$ 710.00
100 mg
$ 1,100.00
200 mg
$ 1,470.00
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