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LSD1 demethylation

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-149213
    LSD1/TLK1-IN-1

    J54; J3-54

    		 Histone Demethylase TLK Cancer
    LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, acts as a weak D4R antagonist, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation, shows minimal toxicity, and has no significant effect on normal prostate cells. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
    LSD1/TLK1-IN-1
  • HY-123577
    TPC-144

    		Histone Demethylase Apoptosis Cancer
    TPC-144 is a LSD1/KDM1A inhibitor. TPC-144 inhibits LSD1, and leads to a decrease in the protein level of DNMT1, causing low methylation of the LINE-1 element. TPC-144 can also produce a synergistic effect with Decitabine (HY-A0004) (a DNMT inhibitor), jointly promoting DNA demethylation and thereby inducing differentiation and apoptosis of leukemia cells. TPC-144 has also demonstrated anti-tumor efficacy in acute myeloid leukemia (AML) models. TPC-144 can be used for the study of AML .
    TPC-144
  • HY-161849
    LSD1-IN-31

    		Histone Demethylase Metabolic Disease
    LSD1-IN-31 (compound 11e) can directly bind to LSD1/CoREST complex to reduce LSD1 demethylation enzymatic activity. LSD1-IN-31 inhibits LSD1 demethylation activity and influences its downstream IκB/NF-κB signaling pathway. LSD1-IN-31 inhibits osteoclastic bone loss in vitro and in vivo. LSD1-IN-31 can be used for osteoporosis research .
    LSD1-IN-31
  • HY-161848
    TCP-MP-CA

    		Histone Demethylase Cancer
    TCP-MP-CA (compound 11a) is an inhibitor of LSD1 demethylation enzymatic via binding to LSD1/CoREST complex. TCP-MP-CA exhibits an inhibitory effect on osteoclastogenesis, with an IC50 value of 0.14 µM .
    TCP-MP-CA
  • HY-168086
    LSD1-IN-35

    		PD-1/PD-L1 Histone Demethylase Infection Inflammation/Immunology
    LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction .
    LSD1-IN-35
  • HY-173590
    AW4

    		Histone Demethylase Cancer
    AW4 is a LSD1 inhibitor. AW4 inhibits LSD1 ΔTTAS activity in H3K4me2 demethylation assays. AW4 can be used for research of drug resistance .
    AW4

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