PIM-1/HDAC-IN-2

PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; HDAC; PARP; Pim

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C1N(C(NC2CCN(CC2)CC3=CC=C(C=C3)/C=C/C(NO)=O)=NC4=C1C=CC=C4C5=CC6=C(N5)[C@H](NC6=O)C)C7(C)CC7

Molecular Formula

C34H37N7O4

Molecular Weight

607.70

References & Citations

[1]Xin Y, et al. Rational Design of Novel Quinazolinone-Pyrrolodihydropyrrolone Analogs as PIM/HDAC Dual-Target Inhibitors for the Treatment of Acute Myelocytic Leukemia. J Med Chem. 2025 Jun 12;68 (11) :11062-11080.