There are two classes of enzymes involved in histone methylation: methyltransferases and demethylases. While methyltransferases are responsible for establishing methylation patterns, demethylases are capable of removing methyl groups not only from histones but other proteins as well. Histone demethylases not only target methylated sites on histone tails but also interact with methylated sites on non-histone proteins, such as p53.
Histone lysine demethylases (KDMs) are of interest as drug targets due to their regulatory roles in chromatin organization and their tight associations with diseases including cancer and mental disorders.
JMJD1A (also named KDM3A) is a demethylasethat removes methyl from histone lysine H3K9. It plays important roles in various cellular processes, including spermatogenesis, energy metabolism, regulation of stem cell and gender display.
Jumonji domain-containing 3 (Jmjd3) has been identified as a histone demethylase, which specifically catalyzes the removal of methylation from H3K27me3.
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9601 |
MC2652 |
1228143-79-0 | MC2652 is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells. |
H9409 |
TAK-418 |
1818252-53-7 | TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM; TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models. |
H9067 |
CC-90011 |
2097523-60-7 | CC-90011 (Pulrodemstat tosylate)is a potent and selective reversible inhibitor of lysine specific demethylase 1 (LSD1) with IC50 value of 0.3 nM;And induction of on-target cellular differentiation marker CD11b in THP-1 cell line with EC50 = 7 nM, antiproliferative activity in AML kasumi-1 cells with EC50 = 2 nM, and no effect in normal human fibroblasts (IMR-90). |
H9066 |
CC-90011 free base |
1821307-10-1 | CC-90011 free base is a potent and selective reversible inhibitor of lysine specific demethylase 1 (LSD1) with IC50 value of 0.3 nM;And induction of on-target cellular differentiation marker CD11b in THP-1 cell line with EC50 = 7 nM, antiproliferative activity in AML kasumi-1 cells with EC50 = 2 nM, and no effect in normal human fibroblasts (IMR-90). |
H8932 |
Bomedemstat |
1990504-34-1 | Bomedemstat(IMG 7289) is a potent,orally administered Lysine Specific Demethylase 1(LSD1) inhibitor. |
H2701 |
Vafidemstat |
1357362-02-7 | Vafidemstat is a novel potent, selective lysine-specific histone demethylase (LSD1) inhibitor. |
H2700 |
T-448 free base |
1597426-52-2 | T-448 free base (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts; increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction, shows unique therapeutic approaches for central nervous system disorders associated with epigenetic dysregulation. |
H2699 |
T-448 |
1597426-53-3 | T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts; increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction, shows unique therapeutic approaches for central nervous system disorders associated with epigenetic dysregulation. |
H2698 |
T-3775440 hydrochloride |
1422535-52-1 | A novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM; displays high selectivity for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B); disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B) in leukemia cell lines, exhibites significant antitumor efficacy in AEL and AMKL xenograft models. |
H2697 |
T-3775440 |
1422620-34-5 |
T-3775440 is a novel potent, selecitve, irreversible LSD1 inhibitor with IC50 of 2.1 nM; displays high selectivity for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B); disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B) in leukemia cell lines, exhibites significant antitumor efficacy in AEL and AMKL xenograft models. |
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