γ-Fibrinogen377-395 is a fibrinogen-derived inhibitory peptide, as well as fibrinogen epitope. γ-Fibrinogen377-395 blocks microglia activation and inhibits fibrin-Mac-1 interactions in vitro, and suppresses experimental autoimmune encephalomyelitis (EAE) in mice in vivo. γ-Fibrinogen377-395 can be used for research in multiple sclerosis (MS), and other neuroinflammatory diseases associated with blood-brain barrier disruption and microglia activation[1].
Rifaximin(Xifaxan) is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity.IC50 Value:Target: RNA polymerase; antibacterialRifaximin is a semisynthetic, rifamycin-based non-systemic antibiotic, meaning that very little of the drug will pass the gastrointestinal wall into the circulation as is common for other types of orally administered antibiotics. It is used in the treatment of traveler's diarrhea and hepatic encephalopathy, for which it received orphan drug status from the U.S. Food and Drug Administration in 1998. Rifaximin interferes with transcription by binding to the β-subunit of bacterial RNA polymerase. This results in the blockage of the translocation step that normally follows the formation of the first phosphodiester bond, which occurs in the transcription process. From Wikipedia.
Stilbamidine is a diamidine compound derived from Stilbene and used chiefly in the form of its crystalline isethionate salt in treating various fungal infections.
Tenuifoliside B, a component isolated from Polygalae Radix, inhibits potassium cyanide (KCN)-induced hypoxia and scopolamine-induced memory impairment. Tenuifoliside B shows potential cognitive improvement and cerebral protective effects. Tenuifoliside B has potential to become an anti-AD lead compound[1][2].
DNP-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Lysyl endopeptidase (Lys-C) catalyzes carboxyl oxygen exchange reaction. Lysyl endopeptidase has higher substrate binding affinities and higher catalytic rates at the acidic pHs than at the alkaline pHs[1].
MNS is a potent and selective inhibitor of Src and Syk tyrosine kinases. target: src, syk. [1]IC50:29.3 (src), 2.5 uM (syk); [1]In vitro: no direct effects on protein kinase C, Ca2+ mobilization, Ca2+-dependent enzymes, PKC activation. MNS potently prevents GPIIb/IIIa activation and platelet aggregation without directly affecting other signaling pathways required for platelet activation. [1] [2] MNS is much more potent than genistein in inhibiting platelet aggregation and protein tyrosine phosphorylation. [2]
(E/Z)-4,4'-Dicyanostilbene is the inactive isomer of 4,4'-Dicyanostilbene (HY-W112166A), and can be used as an experimental control. 4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC50 of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA)[1].
N-Boc-MeVal is an ADC linker with BOC protecting group[1].
Lacutoclax is a Bcl-2 inhibitor with antineoplastic activity[1].
Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities[1][2].
PNU-103017 is an HIV protease inhibitor.
[Tyr4]-Bombesin is a Bombesin analogue, is a ligand of gastrin-releasing peptide receptor (GRPR)[1].
Zearalenone is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds. Possess oestrogenic activity in pigs, cattle and sheep, with low acute toxicity. Causes precocious development of mammae and other estrogenic effects in young gilts[1][2].
2,3-Dihydroxy-4-methoxybenzoic acid is a compound isolated from extracted from sweet cherry fruits (Prunus avium)[1].
Brevinin-2EC is an antimicrobial peptide derived from the skin secretions of Rana esculenta[1].
Fmoc-azetidine-3-carboxylic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-azetidine-3-carboxylic acid is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2].
Coronarin D is a cytotoxic labdan-type diterpenes compound isolated from the rhizomes of H. coronarium[1].
Micromarin F (compound 9) is synthesized from osthole. Micromarin F against Balanus albicostatus and Bugula neritina with EC50 values of 10.93 and 12.38 μM[1].
AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020)[1].
Guanosine 5'-triphosphate-5'-adenosine, the 5′ cap analog, is a fluorescent substrate analog[1].
(S)-Methyl 2-((tert-butoxycarbonyl)amino)-3-methylbutanoate is a valine derivative[1].
Chlophedianol (Clofedanol) hydrochloride is an orally active and potent antitussive agent. Chlophedianol hydrochloride can be used for the research of acute cough due to upper respiratory tract infections (URIs)[1][2].
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer[1].
Epiberberine chloride, a natural alkaloid, is a BACE1 inhibitor, which also exhibits inhibition activity on CYP2D6 and aldose reductase, alpha-adrenoceptors, acetylcholinesterase (AChE), butyrylcholinesterase, and b-site amyloid precursor protein cleaving enzyme 1.
Boc-C2-NH2 is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Glycolate oxidase-IN-1(compound 26), a salicylic acid derivative, is a glycolate oxidase (GO) inhibitor with an IC50 of 38.2 μM. Glycolate oxidase-IN-1 has the ability to reduce oxalate production in hyperoxalate hepatocytes and can be used in the study of primary hyperoxaluria type 1 (PH1)[1].
Tigulixostat is a novel (indolyl)heteroarylcarboxylate derivatives effective as non-purine selective xanthine oxidase inhibitor, which lowers the production of uric acid[1].
Taragarestrant (D-0502) is a potent, orally active estrogen receptor degrader. Taragarestrant has antiproliferative activity against estrogen receptor-positive breast cancer cell lines and has anticancer activity. Taragarestrant can be used for cancer research[1][2].
MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.