Regulator Proteins

Although the mechanisms of action of a number of Axon Ligands™ remain ambiguous, they can significantly affect biological processes of various kinds. While interacting with regulator proteins in this section, they may have therapeutic applications as their target proteins play a role in the regulation and/or facilitation of processes within the cell, without having enzymatic or transporting properties by themselves. Additionally, their mode of action may not have been elucidated in great detail, yet evidence has been found for a certain role in, for example:  signaling pathwaysapoptosis, or stem cell differentiation.
Calmodulin (CaM) is a ubiquitous regulatory protein that communicates the presence of calcium to its molecular targets and correspondingly modulates their function. This key signaling protein is important for controlling the activity of hundreds of membrane channels and transporters[1]. CaM contains two globular domains each containing a pair of helix-loop-helix Ca2+-binding sites (EF-hands). Upon Ca2+ binding, conformational transitions in calmodulin are induced that changes its affinity to target proteins[2]. One example of the proteins function being regulated by CaM is the family of auqaporins (AQPs): water channels that facilitate the flux of water molecules across membranes. Regulation of the water permeability by CaM is achieved through a Ca2+-dependent interaction between Ca2+-CaM and the cytoplasmic C-terminal domain of the AQP[3].
Avridine (Axon 2099),  for example, is a lipoidal amine with interferon-inducing and adjuvant properties specifically related to Newcastle disease[4]. What’s more, although avridine is a synthetic non-immunogenic adjuvant, it is also known to induce arthritis in rats in a predictable and T-cell dependent way. However, the mechanism of action by which this Avridine Induced Arthritis (AvIA) is triggered, or acts as adjuvant of the Newcastle disease antigen has not been elucidated in detail[5].

[1] S.L. Reichow et al. Allosteric mechanism of water-channel gating by Ca2+-calmodulin. Nat. Struct. Mol. Biol. 2013, 20, 1085-1092.
[2] N.V. Valeyev et al. Elucidating the mechanisms of cooperative calcium-calmodulin interactions: a structural systems biology approach.BMC Systems Biol. 2008, 2, 48.
[3] S.L. Reichow et al. Allosteric mechanism of water-channel gating by Ca2+–calmodulin. Nat. Struct. Mol. Biol. 2013, 20, 1085-1092.
[4] M.M. Rweyemamu et al. Efficacy of avridine as an adjuvant forNewcastle disease virus antigen in chickens. Am. J. Vet. Res. 1986, 47, 1243-1248.
[5] C. Vingsbro, R. Jonsson, R. Holmdahl. Avridine-induced arthritis in rats; a T cell-dependent chronic disease influenced both byMHC genes and by non-MHC genes. Clin Exp Immunol 1995, 99, 359-363.

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Axon ID Name Description From price
3755 (+)-Abscisic acid LANCL2 ligand €90.00
1989 (+)-JQ1

Potent and selective BET bromodomain inhibitor

3822 (+)-JQ1 carboxylic acid (+)-JQ1 derivative; PROTAC precursor €110.00
3873 (-)-JQ-1 Inactive enantiomer of (+)-JQ1 €120.00
2830 (R)-CE3F4 Potent inhibitor of EPAC1 €120.00
3928 (R)-SKBG-1 Covalent RNA-binding protein NONO ligand  Recently added €160.00
3929 (S)-SKBG-1 Inactive enantiomer of (R)-SKBG-1  Recently added €150.00
3617 1R,3R-RSL3 (negative control) Negative control of 1S,3R-RSL3 as GPX4 inhibitor €90.00
3957 A-1155463 dihydrochloride BH3 mimetic Ligand of BCL protein BCL-XL Inquire
4008 A-1210477 Potent and selective inhibitor of MCL-1 Inquire
3972 A-1331852 BH3 mimetic Ligand of BCL protein BCL-XL €120.00
3696 ABBV-075 Highly potent and orally bioavailable BET bromodomain (BRD) inhibitor €110.00
3956 ABBV-744 First-in-class highly BDII (Bromodomain II)-selective BET bromodomain inhibitor Inquire
3631 ABR-238901 Potent S100A8/A9 blocker €170.00
2141 ABT 199 Potent, orally bioavailable BCL-2-selective inhibitor €70.00
3821 ABT-263 Potent, selective and orally bioavailable inhibitor of B-cell lymphoma-2 (BCL-2) family proteins Inquire
3687 ADU-S100 Cyclic dinucleotide (CDN) agonist (activator) of Stimulator of Interferon Genes (STING) Inquire
3686 AMG-176 Potent and selective Mcl-1 inhibitor €490.00
3433 ARB-272572 Potent, cellular active PD-L1 inhibitor €150.00
3944 ARV-825 Potent and selective protein BRD4 degrader Inquire
2099 Avridine Lipoidal amine; interferon-inducing and adjuvant properties €80.00
3814 AZD4320 BH3-mimetic inhibitor of BCL-2 protein Inquire
3833 AZD5153 HNT salt Potent, selective, and orally available BET/BRD4 bromodomain inhibitor Inquire
4139 AZD5582 dihydrochloride Apoptosis proteins (IAPs) inhibitor Inquire
3731 AZD5991 BH3-Groove binding Mcl-1 inhibitor Inquire
2185 BAM 7 Selective small-molecule activator of proapoptotic BAX €90.00
2774 Barbadin β-Arrestin/β2-Adaptin inhibitor €120.00
3714 BCL-201 dihydrochloride BH3-mimetic inhibitor of BCL-2 protein Inquire
2624 BF844 CLRN1-N48K stabilizer €105.00
1828 BH3I 1 Inhibitor of Bcl-2 family protein €125.00

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