repression

UNC 669 is an effective and specific MBT (malignant brain tumor) inhibitor with IC50 of 4.2/3.1 uM for L3MBTL1/3.

BRD-K98645985 is a BAF transcriptional repression inhibitor (EC50: ~2.37 µM). It binds ARID1A-specific BAF complexes, potently reverses HIV-1 latency and prevents nucleosomal positioning.

Musk ketone can induce the growth repression and the apoptosis of cancer cells. Musk ketone increases activity of glutathione S-transferase and thus may prove to be useful cancer chemoprotectant.

WK500B is a BCL6 inhibitor that binds to BCL6 within cells, obstructing the BCL6 repression complex and reactivating target genes of BCL6, which leads to the death of DLBCL cells and induces apoptosis and cell cycle arrest. In animal models, WK500B inhibits the formation of germinal centers (GC) and the growth of DLBCL tumors without toxic side effects. Moreover, WK500B demonstrates strong efficacy and favorable pharmacokinetic properties, indicating significant development potential.

(R)-Etodolac is an enantiomer of the non-steroidal anti-inflammatory drug etodolac, known for its ability to inhibit the transcriptional repression of β-catenin. It also exhibits antitumor properties and can be utilized in hepatocellular carcinoma research.

Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm

Robotnikinin is an Shh signaling inhibitor in a concentration-dependent manner. It acts by exhibiting significant repression of Shh-induced Gli1/Gli2.

SR9009 (Stenabolic), a REV-ERB agonist, increases the constitutive repression of genes regulated by REV-ERBα/ERBβ (IC50: 670/800 nM). Through activation of REV-ERB, SR9009 can decrease circadian locomotor activity during the dark phase and alter the expression pattern of core clock genes in the hypothalami of mice. The circadian pattern of expression of an array of metabolic genes in the liver, skeletal muscle, and adipose tissue was also altered in mice exposed to SR9009, resulting in increased energy expenditure. In Diet-induced obese mice, SR9009 (100 mg/kg, i.p., b.i.d., for 30 days) could decrease fat mass and markedly improve dyslipidemia and hyperglycemia.

S-HP210 is a selective glucocorticoid receptor modulator (SGRM) that exerts anti-inflammatory effects by selectively inhibiting NF-κB-mediated transcriptional repression (IC₅₀ = 1.92 μM). At effective doses, S-HP210 exhibits no significant toxicity to mouse 3T3 fibroblasts and effectively inhibits the expression of various pro-inflammatory genes (such as IL-1β, IL-6, and COX-2) induced by LPS.

Glucocorticoid receptor-IN-1 is a selective regulator of the glucocorticoid receptor (GR) and exhibits anti-inflammatory activity. glucocorticoid receptor-IN-1 has good transcriptional repression, acting on hMMP1 ( IC50: 2.11 nM) and also has a transcriptional activating effect on MMTV (EC50: 5.59 nM).

HPPE is a selective inhibitor of Bach1 that acts non-electrophilically. HPPE targets the heme-binding sites on the Bach1 protein and leads to the alleviation of Bach1-mediated repression.

BRD-K25923209 is a novel inhibitor of BAF transcriptional repression.

Nurr1 inverse agonist-1 is a indole-based inverse agonist targeting the neuroprotective transcription factor Nurr1, which plays a pivotal role in dopaminergic neuron regulation. Nurr1 inverse agonist-1 decreases the receptor's intrinsic transcriptional activity by up to more than 90% and revealed preference for inhibiting Nurr1 monomer activity. Nurr1 inverse agonist-1 enables the mechanistic study of Nurr1-mediated gene repression and the exploration of its potential implications in neurodegenerative disorders such as Parkinson’s disease.

Tetraproline, a sequence fragment of tristetraprolin (TTP), facilitates the repression and degradation of mRNAs containing AU-rich elements by recruiting the 4EHP-GYF2 cap-binding complex to TTP's tetraproline motifs [1].

Valproic Acid-D15 is a deuterated compound of Valproic Acid. Valproic Acid (T7064) has a CAS number of 99-66-1. Valproic Acid (T7064) is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid (T7064) have not been completely elucidated. Valproic Acid (T7064) has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid (T7064) is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid (T7064) is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

Valproic Acid-D4 is a deuterated compound of Valproic Acid. Valproic Acid (T7064) has a CAS number of 99-66-1. Valproic Acid (T7064) is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid (T7064) have not been completely elucidated. Valproic Acid (T7064) has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid (T7064) is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid (T7064) is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

2-(Propyl-3,3,3-D3) pentanoic-5,5,5-D3 Acid is a deuterated compound of 2-Propylpentanoic acid (TMSM-3352). 2-pentanoic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

Diflorasone (Standard) is the standard substance of Diflorasone, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Diflorasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. Like other glucocorticoids, diflorasone enters the cell by diffusion across the cell membrane and binds to the glucocorticoid receptor (GR) in the cytoplasm. The receptor complex subsequently translocates to the nucleus and activates or represses genes by interacting with short, palindromic DNA sequences called glucocorticoid response element (GRE). Gene activation leads to the exertion of anti-inflammatory effects, e.g. upregulation of IkappaB, while gene repression inhibits production of pro-inflammatory cytokines such as interleukin-1 (IL-1), IL-2 and IL-6, thereby preventing activation of cytotoxic T-lymphocytes.

Musk ketone (Standard) is the standard substance of Musk ketone, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Musk ketone can induce the growth repression and the apoptosis of cancer cells. Musk ketone increases activity of glutathione S-transferase and thus may prove to be useful cancer chemoprotectant.

Valproic Acid-D15 (Standard) is a reference standard of Valproic Acid-D15 intended for quantitative analysis, quality control, and related biochemical research applications. Valproic Acid-d15 is a deuterated compound of Valproic Acid. Valproic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

Valproic Acid-D4 (Standard) is a reference standard of Valproic Acid-D4 intended for quantitative analysis, quality control, and related biochemical research applications. Valproic Acid-d4 is a deuterated compound of Valproic Acid. Valproic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

2-(Propyl-3,3,3-D3)Pentanoic-5,5,5-D3 Acid (Standard) is a reference standard of 2-(Propyl-3,3,3-D3)Pentanoic-5,5,5-D3 Acid intended for quantitative analysis, quality control, and related biochemical research applications. 2-(Propyl-3,3,3-d3)pentanoic-5,5,5-d3 Acid is a deuterated compound of 2-pentanoic Acid. 2-pentanoic Acid has a CAS number of 99-66-1. Valproic Acid is a branched chain fatty acid which potentially enhances central GABAergic neurotransmission and inhibits Na+ channels. Currently, the various molecular mechanisms of action of Valproic Acid have not been completely elucidated. Valproic Acid has been reported to be a potent inhibitor of histone deacetylases (HDACs) in vitro. Valproic Acid is also noted to relieve HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. Additionally, Valproic Acid is reported to activate Wnt-dependent gene expression and to mimic trichostatin A (sc-3511) in the inhibition of histone deacetylase.

SMRT peptide, one of the corepressor factors interacting with the BCL6 BTB domain, binds to the BTB domain of BCL6 to enhance its transcriptional repression function. Additionally, SMRT peptide is utilized for studying protein-protein interactions.

BCOR(498-514), biotinylated, is the smallest BCL6 binding domain with a KD of 1.32 µM. It can block BCL6-mediated transcriptional repression and induce cell death in lymphoma cells.