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XL-126

Chemical Structure : XL-126

CAS No.:

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XL-126 (XL126)

Catalog No.: PC-21732Not For Human Use, Lab Use Only.

XL-126 (XL126) is a potent BD1-selective BET inhibitor with SPR binding KD value of 8.9 nM, has 185-fold BD1/BD2 selectivity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

XL-126 (XL126) is a potent BD1-selective BET inhibitor with SPR binding KD value of 8.9 nM, has 185-fold BD1/BD2 selectivity.
XL-126 shows an IC50 of 11.9 nM for BRD4 BD1 and a 261-fold selectivity over BRD4 BD2 in TR-FRET assays.
XL-126 demonstrates concentration-dependent inhibition of IL-6 production induces by LPS in murine macrophage J-774 cells (IC50=178 nM).
XL-126 (30 mg/kg, i.p.) exhibits potent anti-inflammatory efficacy, with no significant decrease in platelet count.

Physicochemical Properties

M.Wt 611.77
Formula C33H37N7O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(1-(1,1-Di(pyridin-2-yl)ethyl)-6-(1-methyl-6-oxo-5-(piperidin-4-ylamino)-1,6-dihydropyridin-3-yl)-1H-indol-4-yl)ethanesulfonamide

References

1. Yangfeng Li, et al. J Med Chem. 2024 Jan 31. doi: 10.1021/acs.jmedchem.3c01837.

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