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JBI-589

Chemical Structure : JBI-589

CAS No.: 2308504-22-3

JBI-589 (JBI589)

Catalog No.: PC-49339Not For Human Use, Lab Use Only.

JBI-589 (JBI589) is potent, selective, orally active PAD4 small molecule inhibitor, reduces CXCR2 expression and blocks neutrophil chemotaxis.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JBI-589 (JBI589) is potent, selective, orally active PAD4 small molecule inhibitor, reduces CXCR2 expression and blocks neutrophil chemotaxis.
In vitro, JBI-589 inhibited PMA-induced citrullination of histone H3 in mouse neutrophils in a dose-dependent manner.
JBI-589 demonstrated excellent oral bioavailability with maximum concentration in plasma achieved 0.5h after oral administration and halflife of 6.3h.
JBI-589 significantly and specifically downregulated CXCR2 expression on neutrophil, and reduced their CXCL1-induced migration.
JBI-589 treatment markedly reduced primary tumor growth LL2-bearing and B16F10-bearing mice, also improved the effect of immune checkpoint blockade (ICB).

Physicochemical Properties

M.Wt 481.575
Formula C29H28FN5O
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

[(3R)-3-Amino-1-piperidinyl][2-[1-[(4-fluorophenyl)methyl]-1H-indol-2-yl]-3-methylimidazo[1,2-a]pyridin-7-yl]methanone

References

1. Deng H, et al. Cancer Res. 2022 Oct 4;82(19):3561-3572.

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