h3k9

CMS-121, a quinolone derivative, is an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage (EC50: 7 nM and 200 nM). CMS-121 shows strong neuroprotective, antioxidative, anti-inflammatory, and renoprotective activities.

UNC0224 is a selective inhibitor of G9a with a Ki of 2.6 nM and IC50 of 15 nM. UNC0224 also potently inhibits GLP with assay-dependent IC50 values of 20-58 nM.

UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays.

BRD4770, a histone methyltransferase G9a inhibitor, induces cell senescence.

OSS_128167 (SIRT6-IN-1) is a specific SIRT6 inhibitor, and for SIRT6(IC50=89 μM), SIRT1(IC50=1578 μM) and SIRT2(IC50=751 μM).

ML324(IC50=920 nM) is a specific inhibitor of jumonji histone demethylase (JMJD2).

BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM

Histone H3K9me3 (1-15) (H3(1-15)K9me3) TFA is used as a substrate. This post-translational modification (PTM) of histone H3K9me3 is indicative of heterochromatin surrounding the centromere.

D-α-Hydroxyglutaric acid disodium [Disodium (R)-2-Hydroxyglutarate] is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with a Ki of 0.628 mM.

E67-2, a derivative of E67, is a low-toxicity, selective inhibitor of the KIAA1718 Jumonji domain. It has an IC 50 value of 3.4 μM. E67-2 specifically inhibits the Jumonji demethylase for histone H3 lysine 9 (H3K9) and histone H3 lysine 4 (H3K4) demethylase.

BIX-01294 trihydrochloride is an inhibitor of G9a histone methyltransferase.In a cell-free assay, the IC50=2.7 μM for G9a histone methyltransferase.

193 D7 is an orally bioavailable and selective JMJD1C inhibitor with an IC₅₀ of 0.59 μM and a Kd of 1.96 μM. In HTRF assays, it blocks the binding of JMJD1C to the H3K9me2 peptide substrate with an IC₅₀ of 1.47 μM. 193 D7 regulates the fitness of regulatory T cells (Tregs) in the tumor microenvironment via a dual mechanism: it promotes H3K9me2 enrichment to downregulate PD-1 expression and inhibits STAT3 demethylation to enhance STAT3 activation. It exhibits dose-dependent antitumor activity in multiple mouse tumor models, including MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatoma, and CT26 colorectal cancer, and can be used as a tool molecule for selectively targeting intratumoral Tregs in tumor immunity research.

UNC 0631 is a effectvie histone methyltransferase G9a inhibitor (IC50=4 nM).

CM-272 is a dual G9a/DNA methyltransferases (DNMTs) inhibitor.

BIX-01294 is an G9a Histone Methyltransferase inhibitor(IC50 : 1.9 μM).

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases G9a and GLP (IC50s: 6 nM/15 nM for G9a/GLP). UNC0646(UNC 0646) potently blocks G9a/GLP methyltransferase activity in cells (IC50: 10 nM in MCF7 cells) and exhibits low cellular toxicity (EC50: 4.7 μM in MCF7 cells).

SIRT6-IN-5(SIRT6 inhibitor 5) is a potent and selective SIRT6 inhibitor with an IC50 value of 34 μM.SIRT6-IN-5 is immunosuppressive and chemo-sensitizing, increases H3K9 acetylation and glucose uptake in cultured cells, and reduces T-cell proliferation.

HDAC-IN-98 is an inhibitor of HDAC1, HDAC2, and HDAC3, with IC₅₀ values of 41.2 nM, 52.5 nM, and 74.3 nM, respectively. HDAC-IN-98 induces H3K9 acetylation, upregulates p21 expression, causes G2/M phase arrest, and induces apoptosis, making it suitable for research on epigenetic regulation in tumors.

Rodin-A is an orally active, brain-penetrant, and selective inhibitor of the histone deacetylase (HDAC) CoREST complex, exhibiting an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. It enhances acetylation of histone H3K9 and upregulates neuronal gene expression, leading to increased dendritic spine density, co-localization of synaptic proteins (SV2A and PSD95), and improved hippocampal long-term potentiation (LTP), thus providing synaptic protection and repair. Rodin-A is a promising compound for the study of neurodegenerative diseases associated with synaptic dysfunction, particularly Alzheimer's disease.

AC-340 is a potent hybrid molecule functioning as a VDR agonist and HDAC inhibitor. It can significantly induce the expression of VDR target genes such as CYP24A1, with a selectivity for HDAC2 approximately 10 times greater than for HDAC6 (IC50= 0.37 μM). By causing extensive protein hyperacetylation, such as that of tubulin and H3K9/K27, AC-340 enhances VDR superagonism, resulting in increased acetylation levels of H3K27 on VDR target genes. AC-340 is applicable in research related to melanoma.

Rodin-B is an orally active, brain-penetrant, and selective inhibitor of the histone deacetylase (HDAC)-suppressor of transcription factor corepressor element-1 silencing transcription factor (CoREST) complex. It exhibits an IC50 value of 0.50 μM for the CoREST complex, 0.27 μM for HDAC1, and 0.28 μM for HDAC2. Rodin-B enhances the acetylation level of histone H3K9 and upregulates neuron-related gene expression, promoting increased dendritic spine density, colocalization of synaptic proteins (SV2A and PSD95), and improved hippocampal long-term potentiation (LTP), thereby exerting synaptic protection and repair effects. Rodin-B holds potential for research into neurodegenerative diseases related to synaptic dysfunction, particularly Alzheimer's disease.

BRD6688 is a selective HDAC2 inhibitor that acts by enhancing the learning and memory processes

S2157, a potent N-alkylated tranylcypromine (TCP) derivative lysine-specific demethylase 1 (LSD1) inhibitor, enhances H3K9 methylation and concurrently reduces H3K27 acetylation at super-enhancer sites. This compound triggers apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by inhibiting NOTCH3 and TAL1 gene expression. Moreover, S2157 is capable of crossing the blood-brain barrier, effectively eliminating central nervous system (CNS) leukemia in mice models implanted with T-ALL cells.

S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells when xenotransplanted into mice.