KRAS G12C inhibitor 20 is a KRAS G12C inhibitor extracted from patent CN112694475A, example 1[1].
3-Feruloyl-4-caffeoylquinic acidis acaffeoyl, feruloyl quinic acidderivativeisolated fromroasted C.arabica[1].
Imipenem (N-Formimidoyl thienamycin, MK0787), a stable crystalline derivative of thienamycin, is an antibiotic and has the excellent activity against a broad range of gram-positive and gram-negative aerobic and anaerobic bacteria. Imipenem (N-Formimidoyl thienamycin, MK0787) can be used for carbapenem-nonsusceptible and P. aeruginosa biofilm infections [1][2][3].
Staphyloferrin A is a siderophore protein that can be combined with antibiotics to study drug-resistant bacteria that cause skin diseases[1].
Etozolin (W-2900A) is a diuretic agent. Etozolin inhibits fluid and electrolyte reabsorption in the loop of Henle. Etozolin can be used in research of congestive heart failure, hypertension and edema[1].
Luteolin 7-diglucuronide is the major flavonoid isolated from Aloysia triphylla and Verbena officinalis[1].
VPC-18005 inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, and disrupts the ERG binding to DNA. VPC-18005 is a potent inhibitor of luciferase activity[1].
13-Epijhanol (compound 5) is a diterpenoid compound isolated from Grindelia scorzonerifolia[1].
2,3-Dihydro-12,13-dihydroxyeuparin, isolated from Pappobolus species, is a natural product[1].
Tetrapeptide-1 is a bioactive peptide with antioxidant effect and has been reported used as a cosmetic ingredient[1].
HS-PEG5-CH2CH2NH2 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1)[1].
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice[1].
Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium.IC50 value:Target: Tacalcitol modulates immunological and inflammatory processes. Tacalcitol induces nerve growth factor production in epidermal keratinocytes.
Coreopsin is a natural product that can be isolated from Coreopsis tinctoria Nutt. flower. Coreopsin can be used for hypertension and diabetes research[1].
A-425619, a potent and selective TRPV1 receptor antagonist, is effective in alleviating acute and chronic inflammatory pain and postoperative pain[1].
Thiol-PEG12-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
rac-Rotigotine Hcl is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM. IC50 Value: 0.69 nM(Ki)Target: D-2 receptorin vitro: rac-Rotigotine showed high potency (Ki = 0.69 nM) and selectivity for D-2 receptors as compared to its potency and selectivity at various other neuronal receptors (Ki in nM): D-1 (678) dopamine, alpha 1-(534) and alpha 2-(195) adrenoceptor, S1-(6940) and S2-(5900) serotonin and muscarine (2660). Very low activity (Ki greater than 10(-5) M) was seen at the beta-adrenoceptor, A1-adenosine, GABAA and benzodiazepine receptors. Furthermore, rac-Rotigotine inhibited the calcium-dependent release of [3H]dopamine (IC50: 4 nM) and [3H]acetylcholine (IC50: 6.3 nM) from rabbit striatal slices in the nanomolar range. These effects of rac-Rotigotine were mediated through activation of D-2 dopamine autoreceptors and D-2 dopamine heteroreceptors, respectively.in vivo: Presynaptic dopaminergic activity in vivo was measurable as an inhibition of the locomotor activity of mice, and in this model rac-Rotigotine was more effective than apomorphine. Moreover, the effect of rac-Rotigotine could be antagonized by sulpiride but not by yohimbine. rac-Rotigotine was equipotent with apomorphine in inducing circling behaviour in 6-OHDA-lesioned rats. rac-Rotigotine had almost no serotonergic activity in vivo.
Malvidin (chloride) is a bioactive compound isolated from Oryza sativacv. Heugjinjubyeo. Malvidin shows cytotoxicity through the arrest of the G2/M phase of cell cycle and induction of apoptosis. Malvidin can be used for the research of cancer[1].
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice[1].
Coumarin 6, a fluorescent dye, is used as a fluorescent probe in a microparticle drug delivery system to conduct in vivo tracking, cell uptake, and transport mechanism studies of drug delivery systems[1].
HDAC-IN-29 (compound 13b) is a potent pan-HDAC inhibitor. HDAC-IN-29 shows antitumor activity[1].
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].
Tos-PEG2-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
hPL-IN-1 (compound 2t) is a reversible inhibitor of pancreatic lipase (PL) (IC50=1.86 μM) for anti-obesity research[1].
IR 813 perchlorate is a near-infrared (NIR) fluorescent dye (Ex=815 nm, Em=840 nm) and can be used for visualizing regional lymph nodes in mice[1].
Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
MS-PEG3-dodecyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(E)-1α,25-Dihydroxyprevitamin D3 is a structurally related analog of 1α,25(OH)2D3[1].
COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB[1].