hdm

HDM-IN-1 (Compound A4) is an inhibitor of fungal histone demethylase (HDM) that inhibits H3K27me3 in Cryptococcus neoformans and Candida auris, with IC50 values of 134 nM and 12 nM, respectively. It demonstrates inhibitory activity against these fungi by preventing biofilm and capsule formation, with an MIC80 of 0.5-2 μg mL. Additionally, HDM-IN-1 exhibits antifungal activity in ICR mouse models.

HDM-201 succinate is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.

Synthetic and natural alkyl phosphates, also known as phosphoantigens, stimulate the proliferation of γδ-T lymphocytes. Isopentenyl pyrophosphate, and related derivatives including (E)-hydroxy-dimethyl-allyl pyrophosphate ((E)-HDMAPP), are particularly effective activators of γδ-T cells. (E)-C-HDMAPP is the pyrophosphonate form of (E)-HDMAPP. The pyrophosphonate moiety in (E)-C-HDMAPP is much less susceptible to chemical or enzymatic hydrolysis than its pyrophosphate counterpart. As a result, (E)-C-HDMAPP is much more stable in solution and in vascular circulation. (E)-C-HDMAPP possesses comparable activity to (E)-HDMAPP, which is the most potent of the isoprenoid phosphoantigens. (E)-C-HDMAPP stimulates the synthesis of tumor necrosis factor (TNF-α) by γδ-T lymphocytes with an IC50 value of 0.91 nM. (E)-C-HDMAPP also significantly increases the number of circulating γδ-T cells in vivo, in cynomolgus monkeys.

p53-HDM2-IN-1 is a potent inhibitor of the p53-HDM2 protein-protein interaction, with an inhibitory concentration (IC50) of 0.103 μM, and has significant applications in cancer research.

JHDM-IN-1 (Compound 1), a Jumonji C domain-containing HDMs (JHDM) inhibitor, exhibits IC50s of 3.4 μM against JMJD2C, 4.3 μM against JMJD2A, 5.9 μM against JMJD2E, 10 μM against PHF8, and 43 μM against JMJD3, showcasing its inhibitory effectiveness across a spectrum of JHDM enzymes [1].

Rel-HDMP-28 hydrochloride (Compound 2g) is an analogue of methylphenidate, exhibiting selective affinity for the serotonin transporter (SERT) with a binding constant (Ki) of 105 nM [1].

RITA (NSC-652287)(NSC-652287) induced cross-links of both DNA-DNA and DNA-protein with no detectable DNA single-strand breaks. RITA, like nutlin-3, can disrupt the p53 Mdm2 interaction.

Evatanepag (CP-533536 free acid) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

Siremadlin (NVP-HDM 201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.

OD38 is a novel potent and selective receptor-interacting protein kinase 2 (ripk2) inhibitor

PNC-27, an anticancer peptide with an HDM-2-binding domain, exhibits antitumor activity and has potential applications in acute myeloid leukemia research [1] [2] [3].