Mitomycin C
Mitomycin C is also known as 7-amino-9α-methoxymitosane (Carlos de Oliveira and Wilson, 2020). Chemically, Mitomycin C is a small molecule. Its molecular structure is diagrammatically shown in Figure 1.
GW 4869
Chemically, GW 4869 is a small and novel molecule highly specific in its inhibitory action. Its molecular structure is diagrammatically depicted in Figure 1. It is cationic and also hydrophobic in its behavior. GW 4869 inhibits sphingomyelinases (SMase), more specifically neutral sphingomyelinase 2 (N-SMase 2), also termed sphingomyelin phosphodiesterase 3 (SMPD3) (Vuckovic et al., 2017) in a non-competitive and Magnesium ion dependent manner under both conditions, i.e., in vitro and in vivo, with the half-maximal inhibitory concentration (IC 50) of 1 micro-Molar (μM). This inhibition is tissue dependent as GW 4869 does not inhibit neutral sphingomyelinase 2 (N-SMase 2) in the Multiple myeloma (MM) cells (Vuckovic et al., 2017). SMase is a hydrolase thus, when active it catalyzes the hydrolysis of Sphingomyelin that results in the production of phosphorylcholine and lipid ceramide, that is bioactive in nature. As this hydrolysis occurs optimally at the pH value 7, thus these SMases are termed as neutral sphingomyelinase (N-SMase) (Canals et al., 2011).
LL-37
LL-37, which is also known as cathelicidin. Chemically, it is a peptide, i.e., a short sequence of amino acids (AA), which is made up of only 37 amino acids. Its particular sequence of AA (also called the primary structure) is illustrated in Figure 1. As you can see in Figure 1, its primary structure has two leucine residues and “L” is the alphabetical representation of leucine, therefore it is named as LL-37 (Yang et al., 2020). LL-37 has anti-microbial properties against a broad spectrum of pathogenic microbes, like, bacteria (both, gram positive and negative), viruses and fungi (Turner et al., 1998). It is naturally synthesized in the body, upon the microbial invasion (Chen et al., 2018). It links the two major domains of the immune system, i.e., innate and adaptive. It does so by employing the cells of immune system at the site of infection, and thereby stimulating only the specific receptors on these cells. As it regulates the expression of both distinct types of inflammatory cytokines, i.e., pro- and anti-, normal expression and activity of LL-37 is not only essential but critical to normal physiology of the body.
Staurosporine
Staurosporine (Str) (GC15299) is an alkaloid, which has a complex molecular structure comprising of nine fused rings. Its structure is diagrammatically depicted in Figure 1. It is primarily classified as a derivative of Indolocarbazole (Toledo and Lydon).
Thapsigargin
Thapsigargin
Thapsigargin (shortened as Tg) is a small yet structurally complex molecule, that inhibits the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) at the concentration of nano Molar. Tg at this concentration is particularly safe for the other transmembrane pumps It is the extensively studied SERCA inhibitor. The structure of carbon backbone in the Tg is very complex as there lies a fusion of three rings in the heart of its molecular structure.
3-TYP
3-TYP that is also known as 3-(1H-1,2,3-triazol-4-yl) pyridine, is a small molecule. Its molecular structure is presented in Figure 1. It effectively and selectively modulates i.e., inhibits the Sirt3 protein, a mitochondrial enzyme having roles in the regulation of a vast spectrum of the metabolic processes (a collective term for catabolism and anabolism) thus contributes to the body’s overall homeostasis.
MLN4924
It is a small novel synthetic molecule/ compound, highly selective in its action, and can be used to inhibit the NAE. NAE is defined as the NEDD8 activating enzyme. Different studies showed that this small NEDD8 molecule plays an important role in the regulation of the activity of CRLs. These CLRs (cullin-RING E3 ubiquitin ligases) are essential components of cancer biology as they control the turnover of different kinds of proteins.
KRN 7000
KRN 7000, is also known as α-galactosylceramide (α-GalCer). It is a synthetic glycoprotein i.e., having chemically bonded carbohydrate and lipid part (specifically sphingolipid).Its structural formula is diagrammatically shown in Figure 1, while the different components of KRN 7000 are highlighted in the Figure 2. Keep in mind that both the structures in Figure 1 and Figure 2 are of KRN 7000.
MK-2206 dihydrochloride
It is defined as a novel synthetic compound that can be administered orally for the allosteric inhibition of Akt. This novel molecule requires the pleckstrin homology domain for its action and that’s why it acts as a selective inhibitor of Akt. Studies reported that it is equally potent to inhibit the AKt1 and Akt2 enzymes but is almost 5 times less potent to inhibit the Akt3 enzyme.
T-5224
T-5224 is a small molecule that is non-peptidic in nature. It acts as an inhibitor of activator protein/c-Fos (transcription factors) by inhibiting the binding of activator protein AP-1 to the AP binding site, thus showing anti-inflammatory effects. It regulates the gene expressions for the pro-inflammatory cytokines.