water solubility

Alginic acid (Snow acid algin G) is a natural polysaccharide extracted from brown seaweeds with anti-anaphylactic and anti-inflammatory activities. Alginic acid inhibits histamine release and can be used in the food industry.

Octanoic acid (Caprylic acid), found naturally in coconuts and breast milk, is an oily liquid with a slightly unpleasant rancid taste and minimal solubility in water. It is commercially utilized in the production of esters for perfumery and in dye manufacturing.

Hydroxypropyl cellulose (HPC) is a derivative of cellulose with both water solubility and organic solubility, it is used as food additive and sieving matrix for DNA separations.

4-[(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzoic acid is a synthetic compound with potent antitumor activity, high efficiency and selectivity against tumor cells. However, it has poor solubility in water and is potentially toxic at high concentrations.

Biotin-PEG3-acid is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs. This heterobiofunctional biotin PEG derivative contains a carboxylic acid group. The hydrophilic PEG spacer arm imparts water solubility to the biotinylated molecule. [PEG Linkers] may be useful in the development of antibody-drug conjugates and drug delivery methods.

8pyDTZ is a pyridyl diphenylterazine (DTZ) analog and an ATP-independent pyridyl substrate of LumiLuc luciferase, exhibiting spectrally shifted emission and improved water solubility, suitable for in vivo luminescence imaging.

SUN-597 is a selective inhibitor targeting GSK-3α and β isoforms, showcasing inhibition constants (Ki) of 0.3 nM and 0.05 nM, respectively. It disrupts the proliferation pathways of cells, particularly impacting cellular mechanisms implicated in neurodegenerative diseases and various forms of cancer. While demonstrating efficacy in both in vivo and in vitro studies, SUN-597 has limited water solubility, which poses challenges regarding its formulation and administration.

HJ445A is a highly efficient and selective MYOF inhibitor with excellent water solubility, utilized for the treatment of gastric cancer. In gastric cancer cells MGC803 and MKN45, HJ445A exhibits significant antiproliferative properties with IC50 values of 0.16 μM and 0.14 μM, respectively. The compound binds to the MYOF-C2D domain with a KD value of 0.17 μM and hinders the migration of gastric cancer cells by reversing the epithelial-mesenchymal transition (EMT) process. It also inhibits colony formation in MKN45 cells in a concentration-dependent manner. Remarkably, compared to compound 6y, HJ445A's water solubility is improved by approximately 170 times. Moreover, HJ445A demonstrates superior antitumor effects in vivo.

(S, R, S)-AHPC-PEG8-acid is a synthetic PROTAC linker that binds an E3 ligase ligand with a PEG8 linker to facilitate PROTAC drug development. The PEG8 component enhances the compound's water solubility, and the acid group reacts with amine-containing molecules.

Clethodim is a selective herbicide used to control annual and perennial grass species by inhibiting acetyl-CoA carboxylase activity. Clethodim is characterized by high water solubility, low volatility, and limited environmental persistence in soil and aquatic systems, with moderate toxicity to birds, fish, and pollinators such as honeybees, yet relatively low toxicity toward aquatic invertebrates and algae, thereby making it an effective yet environmentally manageable agrochemical.

Fenretinide glucuronide is a metabolite formed through the glucuronidation of Fenretinide. This process enhances the water solubility of Fenretinide and facilitates its excretion. Fenretinide glucuronide shows potential for research in the field of cancer.

(S,R,S)-AHPC-PEG2-NHS ester is a synthetic PROTAC linker that combines the E3 ligase ligand with a PEG linker to enhance PROTAC pharmacology. The NHS ester reacts with amine groups, and the hydrophilic PEG spacer increases water solubility.

Thalidomide-5-(PEG2-amine) is a Thalidomide analogue that includes an E3 ligase ligand substituted with a terminal amine group. The amine group can react with NHS esters or carboxylic acids in the presence of EDC or HATU. The PEG spacer enhances water solubility.

BDP FL-PEG5-acid is a BDP FL acid linker that incorporates a hydrophilic PEG spacer. It is suitable for the synthesis of PROTACs. BDP FL acts as a green fluorescent dye, and the hydrophilic PEG spacer enhances both water solubility and membrane permeability.

SRC-3-IN-1 (compound SI-10) is an inhibitor of steroid receptor coactivator 3 (SRC-3) with an IC50 of 3.3 μM. It features good water solubility, oral bioavailability, and selectivity. SRC-3-IN-1 is applicable for prostate cancer research.

BMS-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by PXR transactivation, poor water so

Epothilone F is a derivative or analogue of Epothilone D. Epothilone F is also an active metabolite of Epothilone D. In molecule of Epothilone F, a hydroxymethyl group is on the thiazole ring. Like taxanes, Epothilone F prevents cancer cells from dividing

Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen exhibits significant antitumor activity against multiple myeloma (MM) cells and has been shown to inhibit angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells, thereby contributing to its antitumor efficacy. At equivalent molar concentrations, both the salt and free forms of Melflufen exhibit comparable biological activity. However, the salt form, Melflufen hydrochloride, typically demonstrates enhanced water solubility and stability, which may contribute to its increased therapeutic potential.

NBI-30545 is a potent corticotropin-releasing factor-1 antagonist with sufficient lipophilicity and water solubility for the treatment of stress disorders.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

Propacetamol Hydrochloride (Propacetamol HCL) is a prodrug of paracetamol (acetaminophen) with improved water solubility. Propacetamol Hydrochloride is an analgesic drug delivered by IV when the oral application of NSAID is not appropriate or contradicted.

10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) is a Paclitaxel derivative with improved pharmacological features and higher water solubility,used in Chinese clinics to treat cancer.

Antitubercular agent-32 is a Benzothiazinone derivative that inhibits Mycobacterium tuberculosis and exhibits good metabolic stability and water solubility. Antitubercular agent-32 can act on decaprenylphosphoryl-β-D-ribose 2'-oxidase (DprE1, IC50: 3.9 μM) and exhibits antitubercular effects.