A mixture of uvaretin and isouvaretin (HY-N10130) exhibits significant antibacterial activity against B. subtilis (EC50 8.7 μM) and S. epidermidis (IC50 7.9 μM).
8-Oxoepiberberine is an alkaloid metabolite in the plasma after oral administration of Zuojin formula, a traditional chinese medicine used to treat gastrointestinal disease[1].
3-Azetidinemethanol hydrochloride, a medical intermediate, can be used in the synthesis of SHP2 inhibitor[1].
N-Carbobenzyloxy--amino-L-alanine is an alanine derivative[1].
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders[1][2].
Tomatidine acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling.
Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[1][2][3].
2-((2,4-Dimethylphenyl)amino)acetic acid is a Glycine (HY-Y0966) derivative[1].
Kanshone H (compound 6) is a sesquiterpene compound isolated from the underground parts of spikenard[1].
HLCL-61 hydrochloride is a first-in-class small-molecule inhibitor of PRMT5. Target: PRMT5in vitro: HLCL-61 shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples, starting at 12 h post-treatment and persisting after 48 h. Treatment of AML cell lines (MV4-11 and THP-1) and primary blasts with HLCL-61 also resulted in a decrease of cell viability. HLCL-61 is also effective in promoting apoptosis in MV4-11 and THP-1 cells after 48 h.[1]
TAO Kinase inhibitor 2 (Example 49) is a TAO Kinase inhibitor (IC50=between 50 and 500 nM). TAO Kinase inhibitor 2 also inhibits KIAA1361 and JIK with IC50s of 50-500 nM[1].
Factor XI-IN-1 (Compound 27) is a factor XI activation inhibitor with an EC50 of 25.14 nM[1].
Ligularine is a natural pyrrolizidine alkaloid compound[1].
Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
TRC-766 is a negative control of RTC-5 (TRC-382). TRC-766 binds protein phosphatase 2A (PP2A) and does not activate the phosphatase[1].
Hexamethylquercetagetin is a polymethoxylated flavone in peels of citrus cultivars.
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport[1].
Bedaquiline is a diarylquinoline antibiotic that inhibits mycobacterial ATP synthase.
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB)[1][2].
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease[1].
Nemoralisin is a natural acyclic diterpenoid[1].
UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC50 of 79 nM. UR-MB108 is stable in blood plasma[1].
Cerulenin, the best known natural inhibitor of fatty acid synthase (FAS), is an epoxide produced by the fungus Cephalosporium caeruleus.
(S,S)-Valifenalate ((S,S)-IR5885) is an acylamino acid fungicide and is used to control a wide range of fungi belonging to the class of Oomycetes. (S,S)-Valifenalate ((S,S)-IR5885) interferes with the cell-wall synthesis thus affecting the growth stages of the pathogens controlled, both outside (on the spores) or inside the plant (on the mycelium)[1].
Cergutuzumab amunaleukin (CEA-IL2v) is a monomeric carcinoembryonic antigen (CEA)-targeted IL-2 variant-based immunocytokine. Cergutuzumab amunaleukin has immunostimulating and antineoplastic activities[1].
Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.IC50 Value: 7 nM [1]Target: Lckin vitro: Lck Inhibitor (compound 25) exhibited good potency in the T-cell receptor-induced IL-2 secretion assay (IL- 2) and also inhibited subsequent T-cell proliferation (T-cell prolif.) in the same human T -cells.in vivo: A once daily dose of 25was administered orally at 10, 30, and 60 mg/kg from day 9 today 17. Paw volume was measured daily from day 9 through day 18. The compound showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg (Figure 6). Based on the measured plasma levels from the three dose groups, the exposure of 25 at the ED50 was estimated to be 2.7 μM·h (Cmax≈ 0.7 μM) [1].Clinical trial: N/A
PRMT5-IN-2 is a rotein arginine methyltransferase 5 (PRMT5) inhibitor extracted from patent WO2018130840A1, compound 3[1].
RS4317 is a topically effective 5-lipoxygenase (5-LO) inhibitor.
Dictyostatin ((-)-Dictyostatin; Dictyostatin 1) is a potent microtubule stabilizing agent. Dictyostatin also is a anti-cancer agent. Dictyostatin shows antiproliferative activity. Dictyostatin has the potential for the research of tauopathies[1][2][3].
Octyl gallate (Progallin O) is widely used as a food additive, with antimicrobial and antioxidant activity[1][2]. Octyl gallate (Progallin O) shows selective and sensitive fluorescent property[2].