GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability[1].
α-Methyl-DL-phenylalanine is a phenylalanine derivative[1].
Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation [1][2].
Myriceric acid B is a potent HIV-1 entry inhibitor targeting gp41. Myriceric acid B is an antitumor agent[1][2].
Indibulin (ZIO 301) , an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis[1].
Levoleucovorin calcium is the calcium salt of Levoleucovorin, which is the enantiomerically active form of folinic acid.IC50 value: Target: Levoleucovorin is used to treat or prevent toxic effects of methotrexate in people who have received methotrexate to treat bone cancer. Levoleucovorin is also used in combination chemotherapy with fluorouracil (5-FU) to treat colorectal cancer that has spread to other parts of the body. This medicine only treats the symptoms of colorectal cancer and does not treat the cancer itself.
Diethyl-pythiDC is an inhibitor of collagen prolyl 4-hydroxylases (CP4Hs).
PC786 is an inhaled respiratory syncytial virus (RSV) L protein polymerase inhibitor. PC786 demonstrates potent antiviral activity against RSV-A (IC50 <0.09 to 0.71 nM) and RSV-B (IC50, 1.3 to 50.6 nM)[1].
Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1)[1].
Cyanidin 3-sambubioside chloride (Cyanidin-3-O-sambubioside chloride), a major anthocyanin, a natural colorant, and is a potent NO inhibitor. Cyanidin 3-sambubioside chloride is a H274Y mutation inhibitor, and inhibits influenza neuraminidase activity with an IC50 of 72 μM. Cyanidin 3-sambubioside chloride inhibits angiotensin-converting enzyme (ACE) activity and has antioxidant, anti-angiogenic and antiviral properties[1][2][3].
Spacer phosphoramidite C3 is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
AMPK activator 11 is an AMP-activated protein kinase (AMPK) activator with nanomolelevel antiproliferation activities against several CRCs. AMPK activator 11 selectively inhibits the RKO xenograft growth along by activating AMPK and upregulating oxidative phosphorylation (OXPHOS) ( mitochondrial metabolism ) and can be used for anti-tumor and metabolic disease research[1].
K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively[1][2].
Lipoamide-PEG3-Mal is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CFSE is a fluorescent dye which can track the cell division.
14-Norpseurotin is a compound isolated from the culture of Aspergillus fumigatus. 14-Norpseurotin significantly induces neurite outgrowth of rat pheochromocytoma cells (PC12) at a 10.0 microM concentration[1].
Isopulegol is one of the main components of ECO (Eucalyptus citriodora oil). ECO has antibacterial activity[1].
Sonelokimab (ALX 0761; M 1095) is a trivalent nanobody comprised of monovalent camelid-derived nanobodies specific to human interleukin (IL)-17A, IL-17F, and human serum albumin VHHs. Sonelokimab has the potential for plaque-type psoriasis research[1][2].
Triheptanoin (Propane-1,2,3-triyl triheptanoate) is a synthetic medium-chain triglyceride (MCT) consisting of three odd-chain 7-carbon (heptanoate) fatty acids on a glycerol backbone. Triheptanoin can be used for the research of inherited metabolic disorders[1].
Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor. Ilaprazole sodium hydrate irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium hydrate is used for the research of gastric ulcers. Ilaprazole sodium hydrate is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2].
Lecanoric acid is a histidine-decarboxylase inhibitor isolated from fungus. The inhibition by lecanoric acid is competitive with histidineand noncompetitive with pyridoxal phosphate. Lecanoric acid did not inhibit aromatic amino acid decarboxylase[1].
Firefly luciferase-IN-1 (compound 48) is a highly potent and reversible inhibitor of firefly luciferase with an IC50 value of 0.25 nM[1].
Fmoc-L-Lys(Dde)-OH is a lysine derivative[1].
3-epi-Digitoxigenin is a triterpene isolated from the leaves and stems of Plumeria frangipani.
Elcatonin (Carbocalcitonin) acetate is a synthetic analog of eel calcitonin. Elcatonin acetate increases bone mineral density, inhibits bone resorption and processes a central analgesic effect[1].
Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex[1]. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM)[2]. Zotatifin induces cell apoptosis[1].
TNIK-IN-5 is an efficient TNIK inhibitor with IC50 of 0.05 μM. TNIK-IN-5 efficiently inhibits Wnt signaling in intact cells. TNIK-IN-5 shows excellent in vitro anti-colorectal cancer activity[1].
3α-Hydroxytirucalla-7,24-dien-21-oic acid is a tirucallane triterpene isolated from the oleoresin of Protium hebetatum Daly[1].
Tylosin Tartrate is an antibiotic with a large macrocyclic lactone ring.Target: AntibacterialTylosin is a bacteriostat food additive used in veterinary medicine. It has a broad spectrum of activity against gram-positive organisms and a limited range of gram-negative organisms. There is no significant evidence that tylosin resistant staphylococci of animal origin have endangered human health. Tylosin is not effective against the gram-negative intestinal flora, which thus does not lead to selection of R-factors by conjugation. From the human medical stand point, there is no reason that precludes the use of tylosin as a fee additive in animal feeds [1]. Minimum inhibitory concentrations for tylosin tartrate and other commonly used antibiotics were determined for 103 isolates. Most (82.61%) of the isolates not exposed to antibiotics in the 3 months before submission were sensitive to tylosin tartrate. These findings suggest that tylosin tartrate warrants further study as a first-line option for the treatment of dogs initially presenting with pyoderma [2].
Tranexamic acid (Transamin) is an antifibrinolytic for blocking lysine-binding sites of plasmin and elastase-derived plasminogen fragments with IC50 of 5 mM. Target: OthersTranexamic acid is a synthetic derivative of the amino acid lysine. Tranexamic acid is frequently used in surgeries with high risk of blood loss such as cardiac, liver, vascular and large orthopedic procedures. Its oral form is now being evaluated for use in outpatient conditions involving heavy bleeding.Toxicity/Adverse event: Rare in general, including gastrointestinal effects, dizziness, fatigue, headache, and hypersensitivity reactions. Use of tranexamic acid has a potential risk of thrombosis.