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.

LN-439A is a novel tetrahydro-β-carboline small molecule that acts as a potent catalytic inhibitor of the BAP1 deubiquitinase. It induces ubiquitination and degradation of the KLF5 transcription factor by binding to the catalytic pocket of BAP1. In basal-like breast cancer (BLBC) models, LN-439A significantly inhibits tumor cell proliferation and migration, induces G2/M phase arrest and apoptosis, and exhibits superior water solubility compared to existing BAP1 inhibitors. Furthermore, inhibition of BAP1 enzymatic activity by LN-439A also destabilizes its substrates, suggesting potential application value in inflammation-related diseases.

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.

Bis-PEG4-NHS ester is a bis-N-hydroxysuccinimide-activated tetraethylene glycol crosslinker. Bis-PEG4-NHS‘s NHS groups selectively condense with primary amines to form stable amide bonds, thereby covalently crosslinking proteins, peptides, or small molecules. The PEG4 moiety in Bis-PEG4-NHS ester confers good water solubility and flexibility to the conjugate, effectively suppresses nonspecific adsorption, and reduces steric hindrance, thereby supporting site-specific, copper-free click chemistry coupling between antibodies and liposomes. Bis-PEG4-NHS ester can be used for the preparation of homogeneous antibody-drug conjugates (ADCs) and the modular construction of PROTAC bifunctional molecules.

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.

Sepantronium bromide (YM-155) is a novel, highly selective Survivin inhibitor with good water solubility, exhibiting pro-apoptotic effects and antitumor activity. Sepantronium bromide is a Survivin inhibitor with an IC50 of 0.54 nM.

EIDD-036 is a C-20 oxime of Progesterone capable of crossing the blood-brain barrier and binding to progesterone receptors (PR) with an IC50 value of 171 nM. It is the active metabolite of EIDD-1723 and has poor water solubility, making rapid administration in acute injuries challenging. EIDD-036 is applicable for traumatic brain injury (TBI) 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.