1-Methyl-2'-O-methylinosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Boc-2-Nal-OH is an alanine derivative[1].
PROTAC IRAK3 degrade-1 is a potent and selective degrader of IRAK3 (IC50 = 5 nM).
POPSO is a zwitterionic buffer, increases osmolality and shows marked inhibition of anion uniport. POPSO inhibits chloride uniport with an IC50 value of 24 mM. POPSO enhances copper uptake and toxicity in alga, impairs mitochondrial inner membrane. The working pH range of POPSO sesquisodium salt is 7.2-8.5[1][2][3].
S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.IC50 value: 18 nM(EC50) [1]Target: S1P1 agonistWhen dosed orally at 1 and 3 mg/kg, the azahydroxymethyl analogue 22(HY-12835) achieved statistically significant lowering of circulating blood lymphocytes 24 h postdose. In rats, a dose-proportional increase in exposure was measured when 22(HY-12835) was dosed orally at 2 and 100 mg/kg. 22 displayed excellent pharmacokinetic parameters with low clearance (CL = 0.11 L/h/kg), long mean residence time (40 h), and good oral bioavailability (F = 67%).
Acid secretion-IN-1 is a polycyclic compound extracted from patent WO2018024188A1, Compound Example 17.4. Acid secretion-IN-1 is synthesized and used in the IDO inhibitor synthetic experiment[1].
Octan-2-yl 2-cyanoacrylate is a cyanoacrylate compound widely used in industry and medicine as a fast-curing glue or tissue adhesive[1].
Carboxyebselen (HOOC-Ebs) is a potent and selective inhibitor of endothelial nitric oxide synthase (eNOS)[1].
BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM.
Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2].
DBCO-PEG2-NHS ester is a click chemistry reagent containing an azide group. DBCO-PEG2-NHS ester is a click chemistry PEG reagent containing NHS ester that is able to react specifically and efficiently with primary amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond. The hydrophilic PEG spacer arm improves water solubility and provides a long and flexible connection that minimizes steric hindrance involved with ligation. DBCO is commonly used for copper-free Click Chemistry reactions. Reagent grade, for research use only[1].
PKH 26 is a lipophilic membrane dye and widely used to determine cell proliferation in heterogeneous cells by flow cytometry. It is a red‐fluorescent dye (Ex/Em=551/567nm)[1][2].
Desvenlafaxine-d6 is deuterium labeled Desvenlafaxine. Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter[1][2].
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity[1][2][3]. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9[2]. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration[3].
Linopirdine (DUP-996) is a potent Kv7 (KCNQ) voltage-gated potassium channels blcoker; blocks KV7.1+7.3 (KCNQ2+3) / M-currents (IC50=4-7 uM) and KV7.1 (KCNQ1) homomeric channels (IC50=8.9 uM); inhibits M-type K+ current, increases acetylcholine release in rat hippocampal CA1 neurons; active in vivo. Alzheimer Disease Phase 1 Discontinued
Styraxlignolide F is a natural compoundisolated from Styrax japonica.
5’-O-(4,4’-Dimethoxytrityl)-3’-O-t-butyldimethylsilyl adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Xylotetraose is a hydrolysis product of Xylan[1]. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose[2]. Xylotetraose can be used for enzyme biochemical analysis[1][3][4].
KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC50 of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC50s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers[1].
Euxanthone, a xanthone derivative, attenuates Aβ1-42-induced oxidative stress and apoptosis by triggering Autophagy. Euxanthone exhibits anti-neoplastic and neuroprotective activities[1][2][3].
Complanatin I is a natural product that can be isolated from Astragalus complanatus[1].
M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer[1].
ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
Aglain C is isolated from A. ponapensis. Aglain C enhances the NF-kB inhibitory activity[1].
ISIS 329993 (ISIS-CRPRx) is an antisense oligonucleotide targeting to C-reactive protein (CRP). ISIS-CRPRx?has been tested in a rodent model of rheumatoid arthritis (RA) and was shown to improve the clinical signs of arthritis
5(S)15(S)-DiHETE is an “activated” intermediate, inhibits platelet aggregation with an IC50 of 1.3 μM. 5(S)15(S)-DiHETE enhances the rate of either LXA4 or LXB4 biosynthesis[1].
SA1-III(KP1) is a bioactive peptide withanti-agingeffect and has been reported used as a cosmetic ingredient[1].
Cyhalofop-butyl is a post-emergence herbicide. Cyhalofop-butyl inhibits acetyl-coenzyme A carboxylase (ACCase) biosynthesis[1].
Blepharotriol is a phenolic triterpene that can be found in Maytenus blepharodes. Blepharotriol shows antimicrobial activity with a MIC value of 8-4 µg/ml for Bacillus subtilis. Blepharotriol shows cytotoxic activity with IC50s of 12.2, >20, >20 µM for HeLa, Hep-2, Vero cells, respectively[1].
RORγ-IN-1 is a RORγ inhibitor extracted from patent US 9481674 B1, has a Ki of <100 nM.