Gibberellin A5 is a plant hormone that promotes floral development [1].
N6-Furfuryl-2-aminoadenosine is a purine nucleoside analogue. 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].
Thalidezine is a novel activator of AMP-activated protein kinase (AMPK). Thalidezine can eliminate anti-apoptotic cancer cells through energy-mediated autophagy death. Thalidezine can be used to study apoptosis intervention [1].
Cyclo(Met-Met) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Uncargenin C is a triterpenoid, which can be isolated from Uncaria rhychophyllo Miq. Jacks. The intermediate of Uncargenin C has anti-leukemia activity, but not itself[1][2].
SAH-SOS1A is a KRas/son of sevenless 1 (SOS1) interaction inhibitor. SAH-SOS1A binds within nucleotide binding pocket of KRas (Kd values ranges from 106 - 176 nM for wild type KRas and KRas mutants). SAH-SOS1A inhibits nucleotide binding to KRas in a concentration dependent manner.
DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively[1].
TNKS1/2-IN-2 (Compound 21) is a potent and selective tankyrases inhibitor. TNKS1/2-IN-2 exhibits IC50 values of 4 nM and 63 nM against TNK1 and TNK2 in the enzymatic assay, respectively. TNKS1/2-IN-2 inhibits proliferation of A549 and H292 cell lines with IC50 values of 39.5 nM and 12.8 nM, respectively. TNKS1/2-IN-2 can be used for the research of cancer[1].
Lansoprazole sodium(AG-1749) is a proton pump inhibitor which prevents the stomach from producing acid.Target: Proton PumpLansoprazole (sodium) is sodium salt form of lansoprazole, lansoprazole, a substituted benzimidizole proton pump inhibitor, on pharmacokinetics and metabolism of theophylline has been studied in healthy adults given oral lansoprazole 30 mg once daily for 11 days. On Days 4 and 11 of 300 mg aminophylline was simultaneously administered orally and blood samples for theophylline analysis were taken over 24 h [1]. Patients in the lansoprazole group were significantly less likely to have a recurrence of ulcer complications than patients in the placebo group (P=0.008). There was no significant difference in mortality between the two groups [2]. lansoprazole (AG-1749) and omeprazole, were found to have significant activities against this organism. The activity of lansoprazole was comparable to that of bismuth citrate, with MICs ranging from 3.13 to 12.5 micrograms/ml, and fourfold more potent than that of omeprazole [3]. Clinical indications: Duodenal ulcer; Esophagitis; Gastroesophageal reflux; Gastrointestinal disease; Helicobacter pylori infection; Peptic ulcer; Stomach ulcer; Ulcer; Zollinger-Ellison syndromeFDA Approved Date: May 10, 1995Toxicity: Symptoms of overdose include abdominal pain, nausea and diarrhea.
(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].
H-D-Glu-OBzl is a glutamic acid derivative[1].
Boc-Glu(OcHex)-OH is a glutamic acid derivative[1].
Clivatuzumab tetraxetan (IMMU107) is a humanized anti-MUC1 monoclonal antibody. Clivatuzumab tetraxetan shows anti-tumor activity. Clivatuzumab tetraxetan has the potential for the research of metastatic pancreatic cancer[1][2].
Magnoloside A (compound 4) is a main phenylethanoid glycoside in Houpo. Magnoloside A can be used in the research of functional dyspepsia (FD)[1].
Liquiritigenin-7-O-β-D-glucopyranosyl-(1→2)-β-D-apiofuranoside (Liquiritigenin-7-apiosylglucoside) is a flavonoid isolated from the roots of Glycyrrhiza, has weaker cytotoxicity against several tumor cells and normal cells[1].
Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology[1].
(R)-2-amino-2-cyclopentylacetic acid is a Glycine (HY-Y0966) derivative[1].
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells[1].
H-Leu-Gly-βNA can be used as a substrate to detect the presence or absence of N-acetyl-BD-galactosaminidase[1].
9-(3-Deoxy-3-fluoro-β-D-ribofuranosyl)-6-[6-(4-morpholinyl)pyridin-3-yl]purine is a purine nucleoside analogue. 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].
PK14105 is a biological evaluation as a potential radioligand for PET studies of PBBS receptors.in vivo binding experiments, in which PK 14105 was injected into rats with unilaterallylesioned striata, demonstrate that PK 14105 rapidly crosses the blood-brain-barrier and that thereis a marked retention of radioactivity in the lesioned striatum not seen in the unlesioned striatum or cerebellar vermis[1]It can also inhibit receptor ligands, calcium channel ligands and co-transporter in all salivary glands. [2]
1,5,6-Trihydroxy-3-methoxyxanthone is a xanthone that can be found in Hypericum perforatum L.. 1,5,6-Trihydroxy-3-methoxyxanthone shows antioxidant activity and cytotoxicity[1].
TAK-243 is a potent and selective ubiquitin-like modifier activating enzyme 1 (UBA1) inhibitor.
Sofosbuvir impurity K, an diastereoisomer of sofosbuvir, is the impurity of sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
1-(3,5,5,6,8,8-Hexamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethanone-d3 is the deuterium labeled 1-(3,5,5,6,8,8-Hexamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethanone[1].
Isophysalin G is a steroid that inhibits NO production induced by Lipopolysaccharides (HY-D1056) in macrophages with an IC50 of 64.01 μM[1].
Fmoc-Val-Cit-PAB is a linker for antibody-drug-conjugation (ADC).
RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth[1].
Histidylmethionine is a biologically active peptide.