3128804-75-8
Chemical Structure
JH-1
- CAS No.: 3128804-75-8
- Formula:C24H24N4O
- Molecular Weight:384.47
InChIKey: GNKDWNZUVGYWLL-UHFFFAOYSA-N
SMILES: OC(C=C1)=CC=C1C2=CC=C3C(N=CN=C3NC4=CC=C(N(CC)CC)C=C4)=C2
Biological Activity: JH-1 is an orally active and selective KDM1A inhibitor (IC50 = 0.035 μM). JH-1 reversibly inhibits KDM1A and blocks histone demethylation; it binds KDM1A intracellularly and elevates H3K4me1/2 methylation levels in a dose-dependent manner. JH-1 induces ferroptosis and apoptosis in esophageal cancer cells, upregulates ACSL4, BAX, and Cleaved‑caspase‑3, downregulates GPX4 and Bcl‑2, and increases ROS and MDA. JH-1 inhibits tumor growth and upregulates ferroptosis and apoptosis markers in the KYSE510 esophageal cancer xenograft model. JH-1 can be used for research related to esophageal cancer[1].
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JH-1 | JH-1 is an orally active and selective KDM1A inhibitor (IC50 = 0.035 μM). JH-1 reversibly inhibits KDM1A and blocks histone demethylation; it binds KDM1A intracellularly and elevates H3K4me1/2 methylation levels in a dose-dependent manner. JH-1 induces ferroptosis and apoptosis in esophageal cancer cells, upregulates ACSL4, BAX, and Cleaved‑caspase‑3, downregulates GPX4 and Bcl‑2, and increases ROS and MDA. JH-1 inhibits tumor growth and upregulates ferroptosis and apoptosis markers in the KYSE510 esophageal cancer xenograft model. JH-1 can be used for research related to esophageal cancer. | |||||||||||||||||||||
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