dm4

DM4 (Ravtansine) can be used in the preparation of antibody drug conjugate and it is an antitubulin agent. It can inhibit cell division.

DM4-SMe is a cytotoxic part of antibody-drug conjugates (ADCs) and a metabolite of antibody-maytansin conjugates (AMCs) and tubulin inhibitors, which can also be stabilized by disulfide bonds or thioether The bond binds to the antibody. The IC50 of DM4-SM

Maytansinoid DM4, a thiol-containing maytansine derivative, is a highly potent cytotoxic moiety utilized in ADC applications.

DM4-SMCC, a non-cleavable drug-linker conjugate for antibody-drug conjugates (ADC), leverages the antitumor efficacy of DM4 (an antitubulin agent) through attachment with the SMCC linker, exhibiting antitumor activity[1].

DM4-SPDP, a drug-linker conjugate, integrates the antitubulin agent DM4 with the linker SMCC, facilitating the creation of antibody drug conjugates[1]. Additionally, SPDP serves as a short-chain crosslinker enabling amine-to-sulfhydryl conjugation, leveraging NHS-ester and pyridyldithiol groups to establish cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].

SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.

DBA-DM4 is a drug-linker conjugate used in antibody-drug conjugate (ADC) synthesis, combining the tubulin inhibitor DM1 with the SPDP linker [1].

Sulfo-SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugates (ADCs) that employs the maytansine-based payload (DM4, an antitubulin agent) connected through the sulfo-SPDB linker.

Sulfo-PDBA-DM4 is a drug-linker conjugate for antibody-drug conjugate (ADC) applications, combining the potent tubulin inhibitor DM4 with the gluthatione-cleavable linker Sulfo-PDBA. This configuration harnesses DM4's cytotoxic potential through Sulfo-PDBA's targeted delivery mechanism.

Lys-Nε-SPDB-DM4 is a drug-linker conjugate that integrates the tubulin inhibitor DM4 with the linker Lys-Nε-SPDB, enabling the formation of an antibody-drug conjugate (ADC).

S-Me-DM4 is an intracellular enzyme S-methylated metabolite of DM4, a maytansinoid with microtubule-depolymerizing properties and potent cytotoxicity, employed as an Antibody-Drug Conjugate (ADC) cytotoxin [1].

DM4-d6 is a deuterated form of DM4, an antimicrotubule agent that inhibits cell division. DM4 is utilized in the preparation of antibody-drug conjugates (ADCs).

KDM4-IN-4 (compound 47) is a potent inhibitor of histone lysine demethylase 4 (KDM4), with a binding constant of approximately 80 μM for the KDM4A-Tudor domain. It inhibits H3K4Me3 binding to the Tudor domain in cellular contexts with an EC50 value of 105 μM, holding potential for anticancer research applications [1].

KDM4-IN-2 is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.

KDM4Ligand-Linker Conjugate 1 is a conjugate comprising a KDM4 target protein ligand and a linker, used in the synthesis of PROTACKDM4 degrader-1.

KDM4ligand-1 is a ligand targeting the protein (histone lysine demethylase KDM4) in PROTACs. It can be utilized for the synthesis of PROTACs.

PROTACKDM4 degrader-1 (Compound 11) is a proteolysis-targeting chimera (PROTAC) degrader specifically designed for KDM4. It effectively degrades KDM4A-C while sparing KDM4D. In esophageal cancer cells, PROTACKDM4 degrader-1 demonstrates strong antiproliferative activity, inducing apoptosis and cell cycle arrest, and inhibits lysine demethylation of histone H3.

KDM4D-IN-3 is a small molecule epigenetic inhibitor targeting KDM4D, with an IC50 value of 4.8 μM.

BDM44768 is an insulin-degrading enzyme (IDE) inhibitor that acts by inducing glucose intolerance.

KDM4C-IN-35 is a novel and selective KDM4C inhibitor.

KDM4-IN-I is a novel inhibitor of KDM4.

KDM4D-IN-1 is a KDM4D inhibitor (IC50: 0.41±0.03 μM).

KDM4-IN-3 is a cell-permeable KDM4 inhibitor that effectively eliminates prostate cancer cells at low micromolar concentrations.

KDM4C-IN-1 is a selective and potent KDM4C inhibitor (IC50: 8 nM) with potential anticancer activity.KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells, and can be used for the study of leukaemia.