Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants[1][2].
3-O-cis-p-Coumaroyl maslinic acid (compound 16) is a natural compound isolated from the ethyl acetate extract of leaves of Miconia albicans.3-O-cis-p-Coumaroyl maslinic acid can inhibit PTP1B, with the IC50 of 0.46 μM, and shows antimicrobial activity on Gram-positive bacteria and yeasts[1][2].
Z-Asp(OtBu)-OH is an aspartic acid derivative[1].
Stachyanthuside A is an ellagic acid glycoside isolated from the leaves of Diplopanax stachyanthus[1].
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research[1].
GSK-2250665A (Compound 13) is a selective Itk inhibitor with a pKi of 9.2.
Lithium citrate reduces excessive intra-cerebral N-acetyl aspartate in Canavan disease[1].
AC1903 is a potent, specific TRPC5 channel inhibitor with IC50 of 14.7 uM; blocks riluzole-activated TRPC5 whole-cell current, but fails to block carbachol (CCh)-induced TRPC4 and OAG-induced TRPC6 currents, even at high micromolar concentrations; pecifically blocks TRPC5 channel activity in glomeruli of proteinuric rats, suppresses severe proteinuria and prevents podocyte loss in a transgenic rat model of FSGS.
N-Succinimidyl 3-(Bromoacetamido)propionate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. N-Succinimidyl 3-(Bromoacetamido)propionate is also a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines. IC50 value:Target: Anticancer agentin vitro: dioscin (1, 2 and 4 μmol/L) could significantly inhibit the viability of LNCaP cells in a time- and concentration-dependent manner. Flow cytometry revealed that the apoptosis rate was increased after treatment of LNCaP cells with dioscin for 24 h, indicating that apoptosis was an important mechanism by which dioscin inhibited cancer [1]. dioscin abrogated AKT phosphorylation, which subsequently impaired RANKL-induced nuclear factor-kappaB (NF-κB) signaling pathway and inhibited NFATc1 transcriptional activity. Moreover, in vivo studies further verified the bone protection activity of dioscin in osteolytic animal model [2]. Dioscin reduced cell death and lactate dehydrogenase (LDH) release in cells subjected to I/R. I/R induced apoptosis and cytochrome c release from mitochondria to the cytosol and this was prevented by dioscin. In support, dioscin decreased Bax but increased Bcl-2 mRNA expression. Dioscin prevented I/R induced dissipation of ΔΨm [3].
LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.IC50 value:Target: SGLT1/2LX4211 enhanced urinary glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic control, including fasting plasma glucose, oral glucose tolerance, and HbA(1c); and significantly lowered serum triglycerides. LX4211 also mediated trends for lower weight, lower blood pressure, and higher glucagon-like peptide-1 levels. In a follow-up single-dose study in 12 patients with T2DM, LX4211 (300 mg) significantly increased glucagon-like peptide-1 and peptide YY levels relative to pretreatment values, probably by delaying SGLT1-mediated intestinal glucose absorption [1]. LX4211-treated mice and SGLT1-/- mice also had increased GLP-1 AUC values, decreased glucose-dependent insulinotropic polypeptide (GIP) AUC values, and decreased blood glucose excursions during the 6 hours after a challenge with oral glucose alone [2].
Lepadin H is a marine alkaloid and ferroptosis inducer. Lepadin H exhibits significant cytotoxicity, promotes p53 expression, increases ROS production and lipid peroxidation, decreases SLC7A11 and GPX4 levels, and upregulates ACSL4 expression. Lepadin H induces ferroptosis through the p53-SLC7A11-GPX4 pathway[1].
DPH is a potent cell permeable c-Abl activator, which displays potent enzymatic and cellular activity in stimulating c-Abl activation.
Propargyl-PEG4-Sulfone-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines[1].
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) is a cyclic RGD peptide which has high affinity to αvβ3. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors[1].
CFL-120 is a potent KRasG12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer[1].
Ruzotolimod is the agonist of TLR7. Ruzotolimod has the potential for the research of HBV, COVID-19 or SARS-CoV-2 infection (extracted from patent WO2021130195A1)[1].
Dehydrotumulosic acid, one of the effective constituents of Poria cocos, was isolated from the chloroform-soluble material of ethanol extract of the fungus. Poria cocos, a popular Chinese medicinal herb of fungal origin, has been included in many combinations with other CM herbs for its traditionally claimed activities of inducing diuresis, excreting dampness, invigorating the spleen and tranquilizing the mind and its modern pharmacological use of modulating the immune system of the body[1].
Pyribencarb is a benzylcarbamate-type fungicide, which is active against a wide range of plant pathogenic fungi. Pyribencarb is a potent Qo inhibitor of cytochrome b. Pyribencarb is especially active against Botrytis cinerea and Sclerotinia sclerotirum[1].
3,5-O-Dicaffeoylquinic acid reverses Trimethyltin-induced learning and memory deficits[1].
Cefadroxil is a broad-spectrum antibiotic of the cephalosporin type, effective in Gram-positive and Gram-negative bacterial infections.
D-(+)-Cellotriose (Cellotriose) is an oligosaccharide, it is an intermediate in the enzyme hydrolysis of cellulose[1].
KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation[1][2].
Dihydrotachysterol is a synthetic analog of vitamin D. Dihydrotachysterol can be used to for the research of hypocalcemia (lack of calcium in the blood) and hypoparathyroidism (lack of parathyroid hormone in the body) [1][2].
DHODH-IN-2 (compound 21d) is a human dihydroorotate dehydrogenase (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC50 value of 8.6[1].
Amenamevir is a helicase-primase inhibitor which has potent antiviral activity against HSVs with an EC50 of 14 ng/mL.
Cyclopiazonic acid (CPA), a neurotoxic secondary metabolite (SM) made by A. flavus, is a nanomolar inhibitor of endoplasmic reticulum calcium ATPase (Ca2+ATPase; SERCA) and a potent inducer of cell death in plants[1].
Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid, also known as ganoderic acid 24. Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid shows high cytotoxicity against cancer cells, such as human lung cancer cells CH27, melanoma cells M21, and oral cancer cells HSC-3[1].
N-(4-Hydroxyphenyl)glycine is a Glycine (HY-Y0966) derivative[1].