hdm

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

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

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.

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

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.

Hdm2 E3ligaseinhibitor 1 (Compound 1) is a reversible inhibitor of Hdm2-mediated p53 protein ubiquitination, with an IC50 of 12.7 μM. It binds to Hdm2, blocking the transfer of ubiquitin catalyzed by Hdm2 from pre-linked Ub-Ubc4 to p53, thereby inhibiting p53 ubiquitination, stabilizing p53 protein in tumor cells, and exerting antitumor activity.

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.

p53-hDM2 cyclic peptide inhibitor 16e is a cell-permeable inhibitor of the p53-hDM2 interaction with an IC50 of 9.24 nM for hDM2. It is applicable in research related to cancers such as breast cancer, colorectal cancer, and cervical cancer.

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.

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].

Furanones (HDMF) are mainly derived from American grape (Vitis labrusca) and its hybrid varieties. As an important aroma compound in fruits, it exhibits strawberry-like aroma characteristics in some wines.

lutidinic acid (2,4-Dicarboxypyridine) is an in vitro and in cell inhibitor, as well as a known inhibitor of the histone lysine demethylases.

Serdemetan (JNJ-26854165) is an orally bioavailable HDM2 antagonist with potential antineoplastic activity.

Antiflammin P2 is a nonapeptide fragment of lipocortin I which has no phospholipase A2 inhibitory and anti-inflammatory activity.

Odatroltide is a nanoscale P-selectin inhibitor that serves as a nano-delivery system for 6,7-dihydroxyl-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid and KPAK to specifically target the thrombus.

H-D-Met-OMe.HCl is an amino acid derivative with extensive applications in life science research.

H-D-MeAla-EtVal-Val-MeLeu-Ala-D-Ala-MeLeu-MeLeu-MeVal-MeBmt(OAc)-Abu-O-CH2-CH2-NHMe is a derivative of cyclosporin A, lacking immunosuppressive properties, with potential applications in congenital muscular dystrophy research [1].

1-Hexadecyl-3-methylimidazolium hexafluorophosphate (C16mimPF6) is an ionic liquid characterized by a long alkyl-chain imidazolium structure. It is utilized in the creation of inclusion complexes with β-cyclodextrin, and as an electrolyte additive in aluminum-air batteries. When incorporated into phosphatidylcholine (PC) vesicles at concentrations of 10-30 mol%, it reduces particle size and turbidity while enhancing zeta potential. Furthermore, PC vesicles with C16mimPF6 exhibit a lower cytotoxic effect on HaCaT, A431, and SCC-25 cells compared to those with 1-hexadecyl-3-methylimidazolium bromide (C16mimBr).

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.

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].