Chromatin/Epigenetics

MAT2A-IN-21 (compound 28) is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A), with an IC50 of 49 nM. It selectively inhibits cancer cells with MTAP deficiency.

MAT2A-IN-19 (Compound I-3) is an inhibitor of methionine adenosyltransferase 2A (MAT2A), with an IC50 of 32.93 nM.

MAT2A-IN-20 (Compound A49) is an inhibitor of methionine adenosyltransferase 2A (MAT2A) with an IC50 of ≤50 nM. It also inhibits human UGT1A1 with an IC50 of 28.45 μM. Additionally, MAT2A-IN-20 exhibits antitumor activity in mouse models.

MAT2A-IN-17 is a potent inhibitor of MAT2A, with an IC50 of less than 100 nM. MAT2A-IN-17 is applicable in cancer research.

DN02: a potent, selective BRD8(1) bromodomain probe; Ki=32 nM; 30x more affine than BRD8(2).

PLK1-IN-6: potent, selective PLK1 inhibitor, IC50 = 0.45 nM, hinders cancer cell growth.

Desidustat is an inhibitor of HIF hydroxylase.

CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.

Compound A8, known as JAK2-IN-9, is a selective JAK2 inhibitor with an IC50 of 5 nM.

BET-IN-15 (compound 1) is a potent, orally active inhibitor of BET, demonstrating inhibitory IC50 values of 0.64 nM for BRD4-BD1 and 0.25 nM for BRD4-BD2.

Antitumor Agent-104 (Compound 9) serves as an antineoplastic by impeding DNA repair mechanisms in tumor cells, primarily through the inhibition of PARP1 enzyme

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, functions as a potent and selective inhibitor of JAK1 [1].

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM

STAT3-IN-18 (compound SPP), a platinum (IV) complex featuring an axial ligand from sandalwood, suppresses the JAK2-STAT3 pathway in breast cancer (BC) cells and

BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant.

JAK1-IN-11 (compound 11) serves as a potent inhibitor of Janus kinases, exhibiting nanomolar inhibitory concentrations with IC50 values of 0.02 nM (JAK1) and 0.

Lerzeparib is a PARP (ADP-ribose polymerase) inhibitor that exhibits antineoplastic activity [1].

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3,

DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating

BET-IN-14 is a pan BET inhibitor with an IC50 of 5.35 nM, demonstrating oral activity and anticancer properties [1].

PARP7-IN-16 free base is the freebase form of PARP7-IN-16. As a selective oral inhibitor of PARP-1/2/7, it demonstrates IC50 values of 0.94, 0.87, and 0.21 nM, respectively. This compound is utilized in the research of breast and prostate cancer.

BET BD2-IN-3 (compound I-58), a BET inhibitor specifically targeting the BD2 domain, can be radiolabeled with [11C] for use in positron emission tomography (PET) imaging. PET studies with [11C]BD2-IN-3 in mice have demonstrated appropriate biodistribution in peripheral organs and tissues.