transcription

Ceramides Mixture, an endogenous ceramide, consists of hydroxy and non-hydroxy fatty acid-containing ceramides. It is involved in the regulation of cell cycle arrest, growth inhibition, and modulation of telomerase activity.

Baloxavir (S-033447) is a first-in-class cap-dependent endonuclease inhibitor of the influenza virus polymerase PA subunit.

8-Hydroxyquinoline hemisulfate (Oxyquinoline sulfate) is an antiseptic with mild fungistatic, bacteriostatic, anthelmintic, and amebicidal action

Metarrestin (ML246) is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2.

3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) is a bile acid metabolite that inhibits TH17 cell differentiation by directly binding to the transcription factor RORγt with a Kd of 1.13 μM.

BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.

MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM).

YKL-5-124, a potent, selective and covalent CDK7 inhibitor with an IC50 of 9.7 nM, 1300 nM and 3020 nM for CDK7 Mat1 CycH, CDK2 and CDK9 respectively, displays biochemical and cellular selectivity for CDK7 over CDK12 13.

Cjoc42 is an inhibitor of gankyrin, an ankyrin-repeat oncoprotein whose overexpression has been implicated in the development of many cancer types. cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin, and it restores p53-dependent transcription and sensitivity to DNA damage

ML-60218 is an inhibitor of broad-spectrum RNA pol III with IC50s of 32 and 27 μM for Saccharomyces cerevisiae and human. ML-60218 disrupts already assembled viroplasms and hampers the formation of new viroplasms.

POL1-IN-1 (Compound 3A) can effectively inhibit the transcription of RNA polymerase I in the A375 malignant melanoma cell line but has no effect on polymerase II.

GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 of 0.4 μM and serves as a small molecule chemical probe for studying the cell biology of the nuclear heme receptor Rev-erbα.

20-DEOXYINGENOL is a natual product.

CCG-222740 is an inhibitor of Rho/MRTF pathway

IMT1 (Propanamide, N,N-dimethyl-2-[[4-(2-methylphenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-) has anticancer activity.

NFAT Transcription Factor Regulator-1 is a synthesis inhibitor of IL-2 with an IC50 of 182 nM.

Transcription factor-IN-1 (Compound 4e) acts as an inhibitor of transcription factors. It exhibits anticonvulsant activity by antagonizing pentylenetetrazole (PTZ) with an ED50 of 34.5 mg kg. Additionally, Transcription factor-IN-1 demonstrates antidepressant activity in a rat model.

The signal transducer and activator of transcription 6 fragments is a peptide with the sequence H2N-Ser-Tyr-Trp-Ser-Asp-Arg-Leu-Ile-Ile-OH, MW= 1152.3.

Transcriptional Intermediary Factor 2 (TIF2) (740-753) is a 14-amino acid peptide coactivator, encompassing residues 740-753 of the TIF-2 protein.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Dexamethasone is a glucocorticoid receptor agonist and IL receptor modulator with anti-inflammatory, immunosuppressive, and apoptosis-inducing activities. It inhibits the production of inflammatory miRNA-155 exosomes in macrophages, significantly reduces inflammatory cytokine expression in neutrophils and monocytes, suppresses LPS-induced macrophage inflammation, and induces autophagy. It is commonly used to induce animal models of depression, muscle atrophy, and hypertension, and holds potential in COVID-19 research.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

TBHQ (tert-Butylhydroquinone) is an antioxidant that induces an antioxidant response through the redox-sensitive transcription factor Nrf2.