LY 344864 racemate is a 5-HT1F receptor agonist extracted from patent US 5708187 A.
DOTA-GA(tBu)4 is a macrocyclic chelator used in medical imaging[1].
Febantel is an anthelmintic for veterinary use on dogs, cats, cattle, sheep, goats, pig and poultry against roundworms and tapeworms.Target: anthelmintic compoundFebantel is a veteran anthelmintic (wormer) compound belonging to the chemical class of the benzimidazoles, but is a so-called pro-benzimidazole, i.e. it is transformed into a benzimidazole once it gets into the host's organism. Febantel it is transformed into fenbendazole in the stomach and the intestine of the host, shortly after ingestion. Once transformed its behavior is comparable to the one of fenbendazole.
PPACK II is an irreversible and specific glandular and plasma kallikreins inhibitor[1].
IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively[1].
TMN355 is a potent chemical cyclophilin A inhibitor and reduces foam cell formation and cytokine secretion. TMN355 is used for atherosclerosis[1].
Brodimoprim (Ro 10-5970), a trimethoprim analogue, is an orally active dihydrofolate reductase inhibitor. Brodimoprim is highly active against a broad spectrum of gram-negative and gram-positive bacteria[1].
TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge[1].
Biotin-C5-NHS Ester is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer[1].
Velneperit (S-2367) is a novel neuropeptide Y (NPY) Y5 receptor antagonist.Target: neuropeptide Y receptorVelneperit (S-2367) is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist.
Santin is a flavonol isolated from Dodonaea uscosa[1].
5,8,11-Eicosatriynoic acid (ETI) is a lipoxygenase inhibitor that blocks LTC4 biosynthesis in mast cell tumor cells[1].
Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.
TTP-8307 is a potent inhibitor of the replication of several Rhinoviruses and Enteroviruses, targets the nonstructural protein 3A, inhibits the replication of coxsackievirus B3 (CVB3 Nancy) with EC50 of 1.2 uM; 3A mutations V45A, I54F, and H57Y confer resistance to TTP-8307.
5-Aminouridine can modify nucleobases and can be incorporated into the target DNA. 5-Aminouridine exhibits a wide range of biological activity and it inhibits the growth of tumors, fungi and viruses[1][2][3].
3-Azidopropylamine is a click chemistry reagent containing an azide group. 3-Azidopropylamine can react with the starch sugar of potato starch for complexation and transfection of plasmid DNA[1].
FFA3 agonist 1 (Compound 24) is an agonist of free fatty acid receptor 3 (FFA3). FFA3 agonist 1 regulates the health effect of intestinal microbiota by activating FFA3[1].
HIV-IN-1 (Compound 50) is a potent inhibitor of HIV. HIV-IN-2 has the potential for the research of HIV infection[1].
Papilostatin-2 is an anti-angiogenic peptide. Papilostatin-2 can be used for the research of anti-angiogenic[1].
ACT-709478 is a potent, selective, oral active, and brain penetrating T-type calcium channel blocker, with IC50s of 6.4, 18, 7.5 and 2410 nM for Cav3.1, Cav3.2, Cav3.3, Cav1.2, respectively. ACT-709478 is effective on rat and mice, dog, and cynomolgus T-type calcium channel, with no significant species differences. ACT-709478 is used in the research of generalized epilepsies[1].
Ambazone is an orally active membrane active antitumor agent. Ambazone also shows antibacterial and weak antiviral activities[1].
Phenosulfazole is an effective antiviral agent. Phenosulfazole has the potential for the research of poliomyelitis virus[1].
PDE5-IN-42 (Compound 42) is a potent and orally active PDE5 inhibitor with an IC50 of 0.04 nM. PDE5-IN-42 maintains selectivity over PDE6 and PDE11[1].
Vin-C01 is a potent pancreatic β-cells protective agent with an EC50 of 0.22 µM. Vin-C01 effectively promotes β-cell survival and protects β-cells from STZ-induced apoptosis. Vin-C01 can be used for type 2 diabetes mellitus research[1].
6-Chlorovanillin is identified in waste waters from bleached kraft pulp mills in Ontario and earlier also elsewhere>[1].
Volucrin is a dimeric phenanthrene derivative that can be isolated from the orchid lusia volucris[1].
Methylproamine is a DNA-binding radioprotector which, on the basis of published pulse radiolysis studies, acts by repair of transient radiation-induced oxidative species on DNA.IC50 Value: N/ATarget: DNA-binding radioprotectorin vitro: The extent of radioprotection at the clonogenic survival endpoint increased with methylproamine concentration up to a maximum dose modification factor (DMF) of 2.0 at 10 μM. At least 0.1 fmole/nucleus of methylproamine is required to achieve a substantial level of radioprotection (DMF of 1.3) with maximum protection (DMF of 2.0) achieved at 0.23 fmole/nucleus. The γH2AX focus yield per cell nucleus 45 min after irradiation decreased with drug concentration with a DMF of 2.5 at 10 μM [1]. Methylproamine-treated cells had fewer γH2AX foci after IR compared to untreated cells. Also, the presence ofmethylproamine decreased the amount of lower molecular weight DNA entering the gel as shown by the pulsed field gel electrophoresis assay [2]. Experiments with V79 cells have shown that methylproamine is approximately 100-fold more potent than the classical aminothiol radioprotector WR1065. The crystal structures of methylproamine and proamine complexes with the dodecamer d(CGCGAATTCGCG)(2) confirm that the new analogues also are minor groove binders [3].in vivo: N/AClinical trial: N/A
N-methyl-N'-methyl-O-(m-PEG4)-O'-(propargyl-PEG4)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity[1].