promoters

3,29-O-Dibenzoyloxykarounidiol is a natural product with regulate blood sugar level, has potent inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induced by tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA).

OAC1 (BAS 00287861) is a compound activating Octamer-binding transcription factor 4 (Oct4). It enhances the iPSC reprogramming efficiency and accelerates the reprogramming process.

P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferative effects with significantly higher specificity compared to PRIMA-1 and promotes the recruitment of both wild-type p53 and p53 M237I to various target gene promoters. Additionally, P53R3 markedly increases the mRNA, total protein, and cell surface expression of death receptor 5 (DR5), demonstrating its utility in cancer research.

TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

CTPB is a potent p300 histone acetyltransferase (HAT) activator that can be used in the preparation of hair growth promoters and/or hair loss treatments.

TPO agonist 1 (TPO mimetic) is an effective thrombopoietin (TPO) agonist that promotes platelet and megakaryocyte production, suitable for thrombocytopenia research.

c-MYC/BCL2 ligand 1 iodide is a dual-target ligand that specifically interacts with the G-quadruplex (G4) regions of the c-MYC and Bcl-2 promoters, exhibiting Kd values of 0.90 μM for c-MYCG4 and 0.56 μM for Bcl-2G4. It works by binding to these G4-forming sequences to inhibit transcription of the c-MYC and Bcl-2 genes, leading to reduced protein expression. This compound effectively suppresses MCF-7 cell proliferation and migration, induces G1 phase cell cycle arrest, and triggers apoptosis. Additionally, it significantly hampers tumor growth in the 4T1 homogenous model with negligible toxicity. c-MYC/BCL2 ligand 1 iodide is applicable in breast cancer research.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

Bindarit is a selective inhibitor of monocyte chemoattractant proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8 with anti-inflammatory effects. Bindarit specifically inhibits p65- and p65/p50-induced MCP-1 promoter activation and has no effect on other tested activated promoters.

SN-28049 SN is a DNA intercalating drug that binds selectively to GC-rich DNA and shows curative activity against the Colon 38 adenocarcinoma in mice. SN 28049 has a complex action that may involve poisoning of topo IIalpha, suppression of topo I and inhibition of gene transcription from promoters with SP-1 sites. These actions may contribute to the promising experimental solid tumour anticancer activity of SN 28049.

DB2313 is a first-in-class potent small-molecule inhibitor of PU.1. DB2313 disrupts the interaction of PU.1 with target gene promoters and leads to down-regulation of canonical PU.1 transcriptional targets.

Senexin A hydrochloride functions as a selective inhibitor of CDK8/19, with an IC 50 of 280 nM for CDK8, and specifically inhibits p21-induced transcription without affecting other biological effects of p21. Additionally, it suppresses CMV-GFP induction and the stimulatory activity of the consensus NF-κB-dependent promoters [1] [2].

DB2313 (Carboximidamide) is a potent transcription factor PU.1 inhibitor, IC50=14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects

11-Oxomogroside IIIE (Standard) is a reference standard for research and analysis in studies involving 11-Oxomogroside IIIE. 11-Oxomogroside IIIE is a cucurbitane triterpene glycoside isolated from Siraitia grosvenorii (Lo Han Kuo), a traditional Chinese fruit used as a pulmonary demulcent for conditions including dry cough, sore throat, thirst, and constipation. Triterpenoids from this plant were evaluated for inhibition of Epstein–Barr virus early antigen induction by TPA in Raji cells, a primary screen for antitumor promoters, amongst all tested compounds, 11-Oxomogroside IIIE exhibited strong suppression with 70–100% inhibition at 1 × 10³ mol ratio/TPA.

11-Oxomogroside IIIE is a cucurbitane triterpene glycoside isolated from Siraitia grosvenorii (Lo Han Kuo), a traditional Chinese fruit used as a pulmonary demulcent for conditions including dry cough, sore throat, thirst, and constipation. Triterpenoids from this plant were evaluated for inhibition of Epstein–Barr virus early antigen induction by TPA in Raji cells, a primary screen for antitumor promoters, amongst all tested compounds, 11-Oxomogroside IIIE exhibited strong suppression with 70–100% inhibition at 1 × 10³ mol ratio/TPA.

7-Methoxyrosmanol (7-O-Methylrosmanol) can effectively suppress FSK-induced luciferase expression under the control of the CRE, PEPCK-C and G6Pase gene promoters, it may contribute to its antihyperglycemic activity.

Kadsurin has anti-oxidant activity, it induces enzymes capable of scavenging oxygen radical species in the liver. Kadsurin may be valuable antitumor promoters or chemopreventors.

20-Deoxyingenol 3-angelate and ingenol 20-acetate 3-angelate are known as promoters of tumors of mouse skin. 20-Deoxyingenol 3-angelate can induce significant platelet aggregation accompanied by induction of phosphorylation of PKC substrates in platelets,

Interiotherin C may be valuable antitumor promoters or chemopreventors.

CEF27, Epstein-Barr Virus BRLF-1 lytic 148-156 acetate corresponding to amino acids 148-156 of the BRLF1. BRLF1 is a transcriptional activator that binds directly to a GC-rich motif present in some Epstein-Barr virus (EBV) lytic gene promoters.

H3K4(Me) (1-20) is a histone peptide; H3K4me is a complexly regulated post-translational modification closely associated with enhancers and promoters at active transcription genomic sites.