β-Scaffold Factors
Transcription factors (TFs) are key cellular components that control the first step of gene expression, the transcription of DNA into RNA sequences. By ensuring the correct expression of specific genes, the transcriptional regulatory system plays a central part in controlling many biological processes, ranging from cell cycle progression and maintenance of intracellular metabolic and physiological balance, to cellular differentiation and developmental time courses. TFs may be constitutively active or conditionally active. The most common classification of TFs is based on the structure of their DNA-binding domains. Grouping TFs by structural domain has been extremely useful in uncovering how they recognize and bind specific DNA sequences, as well as providing insights into their evolutionary histories. Moreover, in some instances the DNA-binding domain provides clues to their function[1]. A comprehensive classification recognizes four superfamilies with well-defined structural homology: basic domains TFs (1), Zinc-coordinating domains TFs (2), helix-turn-helix (HTH) domains TFs (3), and beta-scaffold domains with Minor Groove Contacts TFs (4). Additionally, a fifth family of orphan TFs exists for which no superclass assignment can be done yet because of lack of structural information[2].
This superfamily of transcription factors with β-scaffold DNA-binding domains with minor groove contacts comprises 11 subclasses: RHR, STAT, p53, MADS box, β-Barrel α-helix transcription factors, TATA binding proteins, HMG-box, Heteromeric CCAAT factors, grainyhead, Cold-shock domain factors, and Runt[2]. Late SV40 Factor (LSF), also known as alpha-globin transcription factor CP2 (TFCP2), functions as part of the SSP(stage selector protein) complex, and binds a variety of cellular and viral promoters including fibrinogen, alpha-globin, SV40 and HIV-1 promoters[3].
[1] J.M. Vaquerizas et al. A census of human transcription factors: function, expression and evolution. Nat. Rev. Genetics 2009, 10, 252-263.
[2] P. Stegmaier, A.E. Kel, E. Wingender. SystematicDNA-binding domain classification of transcription factors. Genome Inform. 2004, 15, 276-286.
[3] P.K. Santhekadur et al. The transcription factor LSF: a novel oncogene for hepatocellular carcinoma. Am. J. Cancer Res. 2012, 2, 269-285.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3834 | Alantolactone | STAT3 inhibitor; NLRP3 inhibitor | €90.00 | |
| 1992 | AS 1517499 | Potent and selective STAT6 inhibitor | €130.00 | |
| 3786 | BP-1-102 | Orally bioavailable STAT3 inhibitor | €90.00 | |
| 2489 | Brassinin | Dual IDO1/STAT3 inhibitor with antifungal and anticancer activity | €75.00 | |
| 3394 | CADD522 | Potent inhibitor of RUNX2-DNA binding | €90.00 | |
| 3035 | Compound 10 |
Tool compound targeting the NFAT:AP-1 transcriptional complex on DNA. |
€150.00 | |
| 2841 | COTI-2 | Reactivator of mutant p53 | €125.00 | |
| 2879 | CP 31398 | Stabilizer of p53 and inducer of apoptosis | €100.00 | |
| 3518 | DCZ0805 | NF-κB activation inhibitor | €130.00 | |
| 2080 | EVP 4593 | NF-κB activation inhibitor; inhibits SOC pathway | €110.00 | |
| 3457 | Fludarabine | Inhibitor of DNA synthesis; STAT-1 activation inhibitor | €50.00 | |
| 2157 | FQI 1 | Inhibitor of α-globin transcription factor CP2 (LSF) | €95.00 | |
| 2349 | JSH 23 | Inhibitor of NF-κB transcription and nuclear translocation of p65 without affecting IκBα degradation | €95.00 | |
| 2378 | Kartogenin | Promotor of chondrocyte differentiation from primary human MSCs | €75.00 | |
| 2319 | L 002 | Inhibitor of p300 HAT (KAT3B) and p53 acetylation | €80.00 | |
| 3270 | Lj-1-60 | Fyn inhibitor targeting the Fyn/Stat3 pathway | €90.00 | |
| 3607 | Micheliolide | NF-κB activation inhibitor | €120.00 | |
| 2517 | Napabucasin | Oral first-in-class cancer stemness inhibitor that works by targeting STAT3 | €105.00 | |
| 3387 | NF-κB Activation Inhibitor IV | Potent NF-κB activation inhibitor | €90.00 | |
| 3909 | NFATc1 inhibitor A04 | Potent RANKL-induced osteoclastogenesis inhibitor | €90.00 | |
| 2016 | NSC 319726 | Reactivator of the p53 mutant p53R175 | €95.00 | |
| 1402 | NSC 348884 | NPM inhibitor | €120.00 | |
| 2564 | NSC 59984 | Activator of p53 that restores WT p53 signaling via p73 activation | €95.00 | |
| 3277 | NSC194598 | p53 DNA-binding inhibitor | €130.00 | |
| 3614 | Parthenolide | NF-κB activation inhibitor | €90.00 | |
| 1871 | Pifithrin-α hydrobromide | Inhibitor of p53 protein | €95.00 | |
| 3051 | Pifithrin-β | Inhibitor of p53 protein; Condensation product of Pifithrin-α | €95.00 | |
| 2488 | Piperlongumine | Natural alkaloid with potent cytotoxic activity | €65.00 | |
| 2313 | S3I 201 | Potent, cellular STAT3 inhibitor | €90.00 | |
| 2244 | SCH 529074 | Small molecule activator of mutant p53. | €120.00 | |