2. シグナル伝達
  3. Epigenetics
  4. Histone Methyltransferase
  5. ASH1L/KMT2H Isoform

ASH1L/KMT2H

ASH1L (absent, small, or homeotic-like 1; KMT2H) is a histone-lysine N-methyltransferase that catalyzes H3K36 methylation, regulating transcriptional elongation and chromatin structure[1][2]. Mechanistically, ASH1L participates in epigenetic programming of neurodevelopment by modulating gene expression critical for neuronal differentiation and synaptic function[1][2]. Dysregulation or loss-of-function variants in ASH1L have been associated with intellectual disability, autism spectrum disorder, and attention deficit hyperactivity disorder, highlighting its role in human neurodevelopmental disorders[1]. Compared with other KMT2 family members, ASH1L exhibits specificity for H3K36 methylation and distinct genomic localization, indicating functional divergence from KMT2A/B/D isoforms[2][3]. In experimental models, ASH1L depletion alters neural progenitor proliferation and differentiation, providing a platform to study neurodevelopmental mechanisms and potential therapeutic targets[1]. While direct small-molecule agonists or inhibitors of ASH1L remain under investigation, modulation of H3K36 methylation indirectly via epigenetic compounds offers a potential approach for mechanistic studies and phenotypic rescue[2][3]. Therefore, ASH1L represents a critical epigenetic regulator with isoform-specific activity and translational relevance in both disease modeling and targeted research applications[1][3].

ASH1L/KMT2H 関連製品 (4):

製品番号 製品名 製品効果 純度
  • HY-141429A
    AS-99 TFA Inhibitor 98.89%
    AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
  • HY-141430
    AS-85 Inhibitor 98.05%
    AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 μM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 μM.
  • HY-141429
    AS-99 free base Inhibitor 98.57%
    AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
  • HY-141429C
    AS-99 Inhibitor
    AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.