ISM012-042

ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS) -induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases[1].

Product Specifications

CAS Number

[2924181-80-4]

UNSPSC

12352005

Target

HIF/HIF Prolyl-Hydroxylase

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

CC(C)(OC(N1CCN(C2=CC=C3C(C=NC(C(NCC4=CN=C(C#N)C=C4)=O)=C3O)=N2)CC1)=O)C

Molecular Formula

C25H27N7O4

Molecular Weight

489.53

References & Citations

[1]Fu Y, et al. Intestinal mucosal barrier repair and immune regulation with an AI-developed gut-restricted PHD inhibitor. Nat Biotechnol. 2024 Dec 11.