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SET-2

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-132222
    SET2

    		TRP Channel Cancer
    SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases .
    <em>SET2</em>
  • HY-131906
    JAK2-IN-7

    		JAK FLT3 Apoptosis Cancer
    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
    JAK<em>2</em>-IN-7
  • HY-144692
    MEK/PI3K-IN-1

    		MEK PI3K PERK Cancer
    MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
    MEK/PI3K-IN-1
  • HY-144693
    MEK/PI3K-IN-2

    		MEK PI3K PERK Cancer
    MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
    MEK/PI3K-IN-<em>2</em>
  • HY-109169
    Bomedemstat

    IMG-7289

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [2].
    Bomedemstat
  • HY-109169A
    Bomedemstat ditosylate

    IMG-7289 ditosylate

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) ditosylate is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat ditosylate can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat ditosylate shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [2].
    Bomedemstat ditosylate
  • HY-109169B
    Bomedemstat hydrochloride

    IMG-7289 hydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) hydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat hydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat hydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [2].
    Bomedemstat hydrochloride
  • HY-109169C
    Bomedemstat dihydrochloride

    IMG-7289 dihydrochloride

    		 Histone Demethylase Apoptosis Cancer
    Bomedemstat (IMG-7289) dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. Bomedemstat dihydrochloride can increase H3K4 and H3K9 methylation, and then alter gene expression. Bomedemstat dihydrochloride shows anti-cancer activities, inhibits cancer cell proliferation and induces apoptosis [2].
    Bomedemstat dihydrochloride
  • HY-155818
    NSD2-IN-4

    		Histone Methyltransferase Cancer
    NSD2-IN-4 is a potent and selective NSD2-SET inhibitor. NSD2-IN-4 has the potential for NSD2-related diseases .
    NSD<em>2</em>-IN-4
  • HY-N5024
    Gambogenic acid
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    Gambogenic acid is an active ingredient that can be isolated from gamboge. Gambogenic acid acts as an effective inhibitor of EZH2, specifically and covalently binds to Cys668 within the EZH2-SET domain, and induces EZH2 ubiquitination. Gambogenic acid can be used for the research of cancer [2].
    Gambogenic acid
  • HY-162308
    NSD-IN-3

    		Histone Methyltransferase Apoptosis Cancer
    NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
    NSD-IN-3
  • HY-101508
    GNA002

    		Histone Methyltransferase Cancer
    GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes .
    GNA002

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