Tavapadon (PF 6649751, PF-06649751) is an orally available dopamine D1 receptor partial agonist for treatment of Parkinson's disease. Parkinson Disease Discontinued
TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research[1].
Sakuranetin is a rice flavonoid phytoalexin, shows strong antifungal activity[1]. Sakuranetin has anti-inflammatory and antioxidative activities. Sakuranetin ameliorates LPS-induced acute lung injury[2].
Boc-Asp-OH is an aspartic acid derivative[1].
FM04 is a potent P-glycoprotein (P-gp) inhibitor (EC50=83 nM). FM04 inhibits P-gp in 2 mechanism: (1)FM04 binds to Q1193, followed by interacting with the functionally critical residues H1195 and T1226; or (2)FM04 binds to I1115 (a functionally critical residue itself), disrupting the R262-Q1081-Q1118 interaction pocket and uncoupling ICL2-NBD2 interaction and thereby inhibiting P-gp[1].
1-(3,4-Dihydroxyphenyl)-7-(4-hydroxyphenyl)hept-6-en-3-ol (Compound 1) is a natural product that can be isolated from rhizomes of Curcuma comosa[1].
MB-0223 is a potent and selective dynamin-related GTPase Drp1 partial inhibitor (IC50=1.3 μM) over other dynamin family members, Opa 1 and dynamin-1 (IC50>100 μM)[1].
Cidofovir dehydrate is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis, which suppresses virus replication by selective inhibition of viral DNA synthesis.Target: CMV DNA polymeraseCidofovir is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis in patients with AIDS. It suppresses CMV replication by selective inhibition of viral DNA polymerase and therefore prevention of viral replication and transcription. It is an acyclic nucleoside phosphonate, and is therefore independent of phosphorylation by viral enzymes, unlike acyclovir.Cidofovir was discovered at the Institute of Organic Chemistry and Biochemistry, Prague, by Antonín Hol?, and developed by Gilead Sciences and is marketed with the brand name Vistide by Gilead in the USA, and by Pfizer elsewhere. Maintenance therapy with cidofovir involves an infusion only once every two weeks, making it a convenient treatment option. Because dosing is relatively infrequent, a permanent catheter is not necessary for infusions.
Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea[1].
Miglustat(OGT918) is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).Target: OthersMiglustat is an inhibitor of the ceramide-specific glycosyltransferase, which catalyzes the first step of glycosphingolipid biosynthesis and is currently approved for the oral treatment of type 1 GD [1]. Consumption of a standard high-fat breakfast within 30 minutes before administration of miglustat significantly reduced peak exposure but did not significantly affect the extent of systemic exposure to miglustat. The peak plasma concentration (C(max)) decreased by 36% on average following administration with food. Area under the plasma concentration-time curve (AUC(0-infinity)) showed a modest (14%) decrease with food, but the 90% confidence interval was within the acceptance limit of 80% to 125%. The median (min-max) time to C(max) (t(max)) was prolonged from 2.5 (1.0-4.0) hours in the fasted state to 4.5 (1.5-8.0) hours in the fed state, whereas the apparent terminal half-life was approximately 8 hours and not affected by food [2].
LG 82-4-01 is a thromboxane (TX) synthetase specific inhibitor, with an IC50 of 1.3 μM[1].
Ethyl 3,4-dihydroxybenzoate (Ethyl protocatechuate), an antioxidant, is a prolyl-hydroxylase inhibitor found in the testa of peanut seeds. Ethyl 3,4-dihydroxybenzoate protects myocardium by activating NO synthase and generating mitochondrial ROS. Ethyl 3,4-dihydroxybenzoate induces cell autophagy and apoptosis in ESCC cells. Ethyl 3,4-dihydroxybenzoate is a collagen synthesis inhibitor and has a bone protecting-effect[1][2][3][4].
Fluorescent DOTAP, a cationic lipid, can be used for the research of nucleic acid and protein delivery[1].
2,16,19-Kauranetriol 2-O-β-D-allopyranoside is an ent-kaurane glycoside, which can be isolated from the fronds of Pteris cretica[1].
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.
Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside is a bioactive constituent that can be found in the seeds of Lepidium apetalum Willd. Isorhamnetin 3-O-β-D-glucose-7-O-β-D-gentiobioside exhibits significant triglyceride (TG)-lowering effects in HepG2 cells[1].
Bis-SS-C3-sulfo-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Temporin F is an antimicrobial peptide against Legionella pneumophila[1].
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity[1][2][3][4][6].
A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC50 values are 18 and 40 nM for rat and human P2X7 receptors, respectively.
Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor. Navitoclax-piperazine and a VHL ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC DT2216 (HY-130604)[1].
Methotrimeprazine (Levomepromazine) is an orally available neuroleptic agent, which is commonly used to relieve nausea and vomiting in palliative care settings. Levomepromazine has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1].
MMP-2/MMP-9-IN-1 is a highly selective, orally active and potent type IV collagenase (MMP-9 and MMP-2) inhibitor with IC50s of 0.24 and 0.31 μM for MMP-9 and MMP-2, respectively. MMP-2/MMP-9-IN-1 is orally active in animal models of tumor growth and metastasis. MMP-2/MMP-9-IN-1 can be used for the research of cancer[1].
(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
1-Fluoronaphthalene is an organofluorine compound derived from naphthalene derivatives and fluorinated aromatics. 1-Fluoronaphthalene can be used to synthesize LY248686, a potent inhibitor of serotonin and noradrenaline uptake[1].
Nandrolone propionate is an anabolic steroid with a relatively long duration of action primarily consisting of androgenic and nitrogen-retentive properties[1].
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase[1].
Tubulin polymerization-IN-7 (compound 5) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-7 has the potential for the research of cancer diseases[1].
SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.