Thapsigargicin (Thapsigargicine) is a activator of mast cells and leukocytes. Thapsigargicin induces histamine release from rat peritoneal mast cells and human basophil leukocytes. Thapsigargicin increases the cytoplasmic free calcium level in intact human blood platelets[1].
TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay[1].
AMG 8379 (AMG-8379, AMG8379) is a potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM; potently blocks endogenous tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglion (DRG) neurons with IC50 of 3.1 nM in whole-cell patch clamp electrophysiology assays; displays100- to 1000-fold selectivity over other NaV family members, including NaV1.4 and NaV1.5; blocks mechanically induced action potential firing in C-fibers, reduces the frequency of thermally induced C-fiber spiking; exhibits pharmacodynamic effects in translatable models of both itch and pain.
Bisacodyl is a stimulant laxative drug that works directly on the colon to produce a bowel movement.Target: OthersBisacodyl is an organic compound that is used as a stimulant laxative drug. Bisacodyl (20 mg/kg) results in a decrease in AQP3 protein expression and increased mRNA expression level of TNF-α in the colon of rats [1]. Bisacodyl inhibits water absorption in rat jejunum, ileum, and colon, the degree of inhibition is linearly related to the logarithm of the bisacodyl concentration over the range of 0.05 mg to 2.0 mg per 100 mL [2]. Bisacodyl (10 mg/kg, intragastrically) induces a significant decrease in jejunal NOS activity in rats. Bisacodyl (10 mg/kg, intragastrically) increases the distance traveled by the marker in all time periods [3]. Bisacodyl (5.9 mg/kg) decreases significantly jejunal and colonic (Na + K) ATPase activity as compared to saline-treated rats. Bisacodyl (5.9 mg/kg) increases significantly jejunal and colonic PGE2 content and stimulates jejunal and colonic adenyl cyclase activity as compared to those in control rats without affecting cAMP content [4]. Bisacodyl (4.3 mg/kg) coupled with AOM increases the number of crypt per focus, but not the number of tumors in rats. Bisacodyl (43 mg/kg) significantly increases the number of crypt per focus and tumors in rats [5].
Daxdilimab is an anti-ILT7 monoclonal antibody, ILT7 is a cell surface molecule specific to the pDC type of dendritic cells. Daxdilimab can be used in acute lung injury (ALI) in patients with COVID-19 infection research[1][2].
(S,S)-TAPI-1 is an isomer of TAPI-1. TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor[1][2].
Ala-Ala-Gln is a peptide. Ala-Ala-Gln can be used for various biochemical studies[1].
Bullatantriol ((+)?-?Bullatantriol) can be isolated from the roots of Homalomena aromatica. Bullatantriol can promote the proliferation and differentiation of osteoblasts. Bullatantriol also inhibits LPS-induced NO production in BV2 cells[1].
SHP2-IN-7 is an SHP2 inhibitor extracted from patent WO2018013597[1].
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively[1]. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA)[2].
JW 642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.IC50 value: 7.6/14/3.7 nM(mouse/rat/human MAGL) [1]Target: MAGL inhibitorJW 642 is selective for MAGL, requiring much higher concentrations to effectively inhibit fatty acid amide hydrolase activity (IC50s = 31, 14, and 20.6 μM for mouse, rat, and human brain membranes, respectively).
Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
S-Methyl-L-cysteine is a natural product that acts as a substrate in the catalytic antioxidant system mediated by methionine sulfoxide reductase A (MSRA), with antioxidative, neuroprotective, and anti-obesity activities.
eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y)[1].
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively[1].
L 655240 is thromboxane antagonist. L 655240 attenuates early ischemia- and reperfusion-induced arrhythmias in a canine model of coronary artery occlusion. L 655240 also involves in cancer and autoimmune disorders[1].
Exendin-4, a 39 amino acid peptide, is a long-acting glucagon-like peptide-1 receptor agonist with an IC50 of 3.22 nM. Sequence: His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2.
TCO4-PEG2-Maleimide is a PROTAC linker and belongs to the PEG class. TCO4-PEG2-Maleimide contains TCO and Maleimide groups, which can undergo specific "click" reactions with tetrazine groups or thiol groups, or "mercapto-acrylamide" reactions.
N1,N1'-(Propane-1,3-diyl)bis(propane-1,3-diamine)-d24 is the deuterium labeled N1,N1'-(Propane-1,3-diyl)bis(propane-1,3-diamine)[1].
Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer[1][2].
Hyperoside, a natural flavonoid, isolated from Camptotheca acuminate, possesses antifungal, anti-inflammatory, anti-viral, anti-oxidative and anti-apoptotic activities[1].
Casirivimab (REGN10933) is a human monoclonal antibody to target SARS-CoV-2 virus, which causes COVID-19. Casirivimab lacks efficacy against COVID-19 variants. Casirivimab can be used in combination with Imdevimab (HY-P99342), it reduces viral load and improves diseases[1].
Monascorubramine is a microbial colorant. Monascorubramine is capable of producing by the Monascus, which is from the bacteria Talaromyces. Under the condition of different pH value, the hue and chromaticity value of the colorant are also different[1].
11-epi-mogroside V is a mogroside in the fruit of Siraitia grosvenori. 11-epi-mogroside V exhibits considerable bioactivity in promoting glucose uptake in human HepG2 cells in vitro [1].
Benzydamine N-Oxide is a metabolite of Benzydamine. Benzydamine N-Oxide can be used to measure flavin-containing monooxygenase activity[1][2].
TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistant Klebsiella pneumoniae and does not pose a cardiovascular risk.
(25R)-Officinalisnin-II (compound 5) is a furostanol glycoside found in the fruits of Asparagus curillus[1].
CID755673 is a potent and selective PKD1 inhibitor with an IC50 of 182 nM.
N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker[1][2]. N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia[3].
R-1479 is a specific inhibitor of HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).