Cap-dependent endonuclease-IN-16 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-16 is a pyridone polycyclic derivative. Cap-dependent endonuclease-IN-16 has the potential for the research of influenza (extracted from patent CN112778330A, compound 15A)[1].
TNKS1/2-IN-1 is a potent tankyrase TNKS1/2 inhibitor with pIC50s ranging from 7.1-8.2. TNKS1/2-IN-1 can be used for research of cancer, fibrosis, and other hyperproliferative diseases[1].
Boc-NH-PEG10-CH2CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(Rac)-Tezacaftor ((Rac)-VX-661) is a racemate of Tezacaftor (HY-15448). Tezacaftor is a F508del CFTR corrector. (Rac)-Tezacaftor can be used for the research of cystic fibrosis[1].
Pradigastat (LCQ-908) is a diacylglycerol acyltransferase 1 (DGAT1) inhibitor.
Cellobiosan-13C is the 13C labeled Cellobiosan[1].
Heparin Binding Peptide is one of the heparin-binding amino acid sequences found in the carboxy-terminal heparin-binding domain of fibronectin.
Triptoquinone A, an interleukin 1 inhibitor, inhibits endomycin (LPS) or interleukin (IL-1β)-promoted induction of nitric oxide synthase (NOS) in vascular smooth muscle, thereby inhibiting Arg-induced vascular relaxation[1].
T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
Nonanoic acid-d2 is the deuterium labeled Nonanoic acid[1]. Nonanoic acid is a naturally-occurring saturated fatty acid with nine carbon atoms. Nonanoic acid significantly reduces bacterial translocation, enhances antibacterial activity, and remarkably increases the secretion of porcine β-defensins 1 (pBD-1) and pBD-2[2].
Taurolithocholic acid-d5 is deuterium labeled Taurolithocholic acid.
MK8033 Hcl is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.IC50 Value: 1 nM (Wt c-Met); 2.0 nM (c-Met N1100Y) [1]Target: c-Metin vitro: MK-8033 binds 3-fold more tightly to phosphorylated c-Met kinase domain (Kd= 3.2 nM) than to its unphosphorylated counterpart (Kd = 10.4 nM). Signigicantly, MK-8033 potently inhibits kinase activity of three oncogenic c-Met activation loop mutants, Y1230C, Y1230H, and Y1235D (IC50s ranging from 0.6 to 1 nM at 50 uM ATP) in addition to other c-Met activating mutants N1100Y and M1250T. MK-8033 potently inhibited GTL-16 proliferation with an IC50 of 582 ± 30 nM. By contrast the HCT116 cell line, which does not harbor basal c-Met activation, was not inhibited by MK-8033 (IC50 > 10000 nM) [1]. MK-8033 radiosensitized the high-c-Met-expressing EBC-1 and H1993 cells but not the low-c-Met-expressing cell lines A549 and H460. However, irradiation of A549 and H460 cells increased the expression of c-Met protein at 30 minutes after the irradiation. Subsequent targeting of this up-regulated c-Met by using MK-8033 followed by a second radiation dose reduced the clonogenic survival of both A549 and H460 cells. MK-8033reduced the levels of radiation-induced phosphorylated (activated) c-Met in A549 cells [2].in vivo: MK-8033 was orally dosed in GTL-16 tumor xenograft bearing mice. Mice were euthanized 1 h after dosing and tested for p-Met (Y1349) in tumors and MK-8033 concentrations in plasma. At 100 mg/kg,essentially complete inhibition of p-Met (Y1349) was achieved. An in vivo IC50 of 1.3 uM was deduced from the relationship between plasma MK-8033 level and Met pY1349. Treatment with escalating dosed of MK-8033 for 21 days lead to antitumor efficacies in a dose-dependent manner. Dosing at 3, 10, 30, and 100 mg/kg resulted in 22, 18, 57, and 86% tumor growth inhibition, respectively, relative to tumor from vehicle-treated mice.
GSK5182 is a highly selective inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM and does not interact with other nuclear receptors, including ERRα or ERα, due to its additional non-covalent interactions with Y326 and N346 at the active site of ERRγ. GSK5182 also induces Reactive Oxyen Species (ROS) generation in hepatocellular carcinoma (HCC)[1][2][3].
Sucrose octasulfate is a component of sulfoaluminum. Sucrose octasulfate stimulates the release of somatostatin-like immunoreactivity (SLI) from the stomach by acting directly on D cells in the gastric mucosa. Sucrose octasulfate exerts its ulcer-healing effect by releasing endogenous gastric somatostatin Sucrose octasulfate can be used for anti-gastric ulcer research [1].
Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU)[1].
PEG 25 cetostearyl ether can be used as an excipient. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1].
Moxetumomab, a recombinant CD22-targeting immunotoxin, can be used for the research of hairy cell leukemia (HCL)[1][2].
X-Gluc Dicyclohexylamine is used as a reagent to detect β-glucuronidase, an enzyme produced by the E. Coli bacterium; is widely used in molecular biology experiments to mark and select the expression of target genes (GUS reporter system).
BO-0742, a derivative of AHMA and N-mustard, is a potent anti-cancer agent. BO-0742 significantly suppresses the growth of xenografts of human breast and ovarian cancers in mice[1].
Fmoc-Gly-Gly-allyl propionate is a cleavable linker that can be used to synthesize Antibody-Drug Conjugates (ADCs).
Penduletin is a flavone, that can be isolated from Brickelia pendula and Vitex negundo. Penduletin shows anticancer activity. Penduletin induces apoptosis in the cancer cells through ROS generation[1][2].
Renchangianin B (compound 2) is dibenzo cyclooctene-type lignan. Renchangianin B can be isolated from the stems of Kadsura renchangiana[1].
Demegestone is an agonist of theprogesterone receptor[1].
DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity[1].
Oxacillin sodium monohydrate is an antibiotic similar to flucloxacillin used in resistant staphylococci infections.Target: AntibacterialOxacillin is a penicillinase-resistant β-lactam. It is similar to methicillin, and has replaced methicillin in clinical use. Another related compound is nafcillin. Since it is resistant to penicillinase enzymes, such as that produced by Staphylococcus aureus, it is widely used clinically in the US to treat penicillin-resistant Staphylococcus aureus. However, with the introduction and widespread use of both oxacillin and methicillin, antibiotic-resistant strains called oxacillin-resistant Staphylococcus aureus (MRSA/ORSA) have become increasingly prevalent worldwide. MRSA/ORSA is treated using vancomycin. From Wikipedia.
PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification[1].
Thioflavine S is a fluorescent histochemical marker of dense core senile plaques.
AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor[1].
Naringenin chalcone is an intermediate in flavonol biosynthesis and is spontaneously metabolized into naringenin (NAR) by chalcone isomerase. Naringenin chalcone has anti-inflammatory and antiallergic activities[1].