A12-Iso5-2DC18 is a potent mRNA delivery lipid vehicle[1].
Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis, reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 μM[1].
Vinblastine is a cytotoxic alkaloid used against various cancer types. Vinblastine inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
Isoboonein (compound 5) is a natural product that can be found in Alstonia scholaris[1].
Clocinnamox (mesylate) is a potent opioid antagonist acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors[1].
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively[1]. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage[2].
Sulfaquinoxaline sodium salt is an antibiotic which has activity against a broad spectrum of Gram-negative and Gram-positive bacteria.
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties[1][2].
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2].
Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity[1].
Flurandrenolone Acetate is a derivative of Flurandrenolide (HY-B1013). Flurandrenolone Acetate is a synthetic glucocorticoid steroid, can be used for the research of skin disorders such as eczema and psoriasis[1].
Euphorblin R (EOF2) is a rhamnyl diterpenoid isolated from Euphorbia resinifera. Euphorblin R may promote lysosomal biogenesis and has the potential to be used in the study of lysosome-related diseases.
N-Desthiobiotin-N-bis(PEG4-NHS ester) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Alpha-mangostin is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
(2R-cis)-5-[Tetrahydro-5-(hydroxymethyl)-4-oxo-2-furanyl]-2,4(1H,3H)-pyrimidinedione 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].
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis[1].
L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min-1[1].
Methyl 2,3-O-Isopropylidene-β-L-ribofuranoside is an enantiomer of Methyl 2,3-O-Isopropylidene-β-D-ribofuranoside. Methyl 2,3-O-Isopropylidene-β-L-ribofuranoside is a derivative of L-ribose[1].
N-Boc-PEG6-alcohol is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) [1].
GW311616A(GW311616 Hcl) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM.IC50 value: 22 nM [1]Target: neutrophil elastaseThe HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin, >3 mM for chymotrypsin and tissue plasminogen activator). Acetylcholinesterase is not inhibited by GW311616A at 100 uM.GW311616A is more potent than thetrifluoromethylketone inhibitor ZD8321 (Ki=13 nM). GW311616A is orallybioavailable in rat, dog (Table 4) and hamster despite moderate to high plasmaclearance, which indicates that clearance is predominantly extrahepatic.
MC-Val-D-Cit-PAB-PNP is a drug-linker-ligand conjugates. MC-Val-D-Cit-PAB-PNP can be used for researching cancer, autoimmune diseases and infectious diseases[1].
TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice[1].
Histidylprolineamide (His-pro-amide) is a reactive amide, an intermediate in the histidine metabolic pathway[1].
VLHDDLLEA is a peptide that can be isolated from the MHC complex HLA-A*0201 molecule. VLHDDLLEA can be recognized by HLA-A*0201-restricted cytotoxic T cells (CTLs). VLHDDLLEA can be used for research on graft versus host disease (GvHD)[1].
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity. Target: Androgen ReceptorCyproterone acetate clearly shows antagonistic properties, while being a partial agonist also, showing agonism for the AR, with EC50 of 4.0 μM, at relatively high concentrations [1]. In the presence of 10 nM Testosterone, low concentrations of Cyproterone acetate inhibits T-stimulated transcription of 3XHRE-LUC, but at higher concentrations, transcription is stimulated. LH levels in Cyproterone acetate-treated rats do not dip below pretreatment levels, although they does not increase as much in the rats treated with 3.2 mg Cyproterone acetate/kg/day as in those which received 0.2 mg Cyproterone acetate/kg/day [2]. Cyproterone acetate exhibits direct negative effect on reproductive organs weight and significant reducing effect on sperm count and Ca2+ contents. SOD and GST activities significantly decrease in addition to significant increase in NO, MDA contents reflecting the oxidative status of testis in Cyproterone acetate treated rats [3].
(1R,2R)-1-Aminoindan-2-ol is the inactive isomer of (1S,2R)-1-Aminoindan-2-ol (HY-W002530), and can be used as an experimental control. (1S,2R)-1-Amino-2,3-dihydro-1H-inden-2-ol is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Py-MAA-Val-Cit-PAB-MMAE (AAJ8D6-PY-Val-Cit-MMAE) is an ADC Linker of Zapadcine-3a. Zapadcine-3a is an anti-TRAILR2 ADC with broad spectrum, and antineoplastic effect. Zapadcine-3a can be swallowed up into lysosome of tumor cells by binding to TRAILR2. Then Zapadcine-3a releases small molecular compound to specifically kill various TRAILR2-pos. Zapadcine-3a potently eradicates tumor cells and cures tumor[1].
Bikaverin (Lycopersin) is a reddish pigment produced by different fungal species. Bikaverin shows antibiotic properties against certain protozoa and fungi[1].