NSC622608 is a first small-molecule ligand for V-domain Ig Suppressor of T-cell Activation (VISTA) with an IC50 of 4.8 μM in TR-FRET assay.
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM[1].
Metolachlor-d6 is the deuterium labeled Metolachlor[1]. Metolachlor is a pre-emergent selective, chloroacetanilide herbicide for the control of a variety of annual grass and broad leaf weeds in corn and other crops. Metolachlor is a chiral herbicide consisting of four stereoisomers[2][3].
PROTAC IRAK4 degrader-7 (Compound I-417) is an orally active PROTAC IRAK4 degrader with antitumor activities[1].
(R)-L 888607 is the inactive isomer of L 888607 (HY-111271), and can be used as an experimental control. L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has high affinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite[1].
ML267 a potent Sfp phosphopantetheinyl transferase (PPTases) inhibitor with an IC50 of 0.29 μM. ML267 also inhibits AcpS-PPTase with an IC50 of 8.1 μM. ML267 possesses specific Gram-positive-targeted bactericidal activities[1].
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity.
N-Decanoyl-DL-homoserine lactone is a serine derivative[1].
Heteroclitin A is a lignan isolated from the stems of Schisandra propinqua.
2-Amino-6-chloropurine-9-beta-D-(2’-deoxy-2’-fluoro)-arabinoriboside 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].
Varespladib methyl is a selective inhibitor of group II secretory phospholipase A2 (PLA2).
L-Glutamic acid potassium salt monohydrate is a glutamic acid derivative[1].
GDC-0334 is a TRPA1 antagonist useful in treatment TRPA1-mediated diseases, such as pain or asthma.
TBA-354 is a potent anti-tuberculosis compound; maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates.IC50 value:Target: Anti-tuberculosis agentin vitro: TBA-354 is narrow spectrum and bactericidal in vitro against replicating and nonreplicating Mycobacterium tuberculosis, with potency similar to that of delamanid and greater than that of PA-824. TBA-354 maintains activity against Mycobacterium tuberculosis H37Rv isogenic monoresistant strains and clinical drug-sensitive and drug-resistant isolates [1]. TBA-354 is 5 to 10 times more potent than PA-824, but selected mutants are cross-resistant to PA-824 and delamanid. TBA-354 is 2 to 4 times more potent than PA-824 when combined with bedaquiline, and when administered at a dose equivalent to that of PA-824, TBA-354 demonstrated superior sterilizing efficacy [2].in vivo: TBA-354 has high bioavailability and a long elimination half-life. In vitro studies suggest a low risk of drug-drug interactions. Low-dose aerosol infection models of acute and chronic murine tuberculosis reveal time- and dose-dependent in vivo bactericidal activity that is at least as potent as that of delamanid and more potent than that of PA-824.
Chondroitin sulfate, one of five classes of glycosaminoglycans, has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs.
LDC1267 is a highly selective TAM(Tyro3, Axl and Mer) kinase inhibitor with IC50 of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.IC50 value: <5 nM/8 nM/29 nM(Tyro3/Axl/Mer) [1]Target: TAM kinase inhibitorin vitro: LDC1267 preferentially inhibits Tyro3,Axl andMer at lownanomolarity, as determined by tracer-based binding assays. Treatment of NKG2D activated NK cells with LDC1267 indeed abolished the inhibitory effects of Gas6 stimulation;LDC1267 had no apparent additional effect in Cbl-b-deficient NK cells. in vivo: wild-type mice treated with LDC1267 showed enhanced cytotoxicity towardsRMAcells overexpressing the NKG2D ligand Rae-1 (RMA-Rae1) to the same extent as C373AKI/KI mice, but had no effect on the already enhanced NK cytotoxicity in Cbl-b-mutant mice. Challenged mice with B16F10 melanoma followedby intraperitoneal LDC1267 treatment. LDC1267 markedly reduced metastatic spreading ofmelanomas; NK1.1 depletion abolished the therapeutic benefits of LDC1267.
H-Phe(3-Cl)-OH is a phenylalanine derivative[1].
Hygromycin B is an aminoglycoside antibiotic active against prokaryotic and eukaryotic cells.
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC)[1].
(((9H-Fluoren-9-yl)methoxy)carbonyl)-L-aspartic acid is an aspartic acid derivative[1].
Metyrosine-13C9,d7,15N is the deuterium, 13C-, and 15-labeled Metyrosine. Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity[1]. Metyrosine is a very effective agent for blood pressure control[2].
2-(Benzyloxy)ethanol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
O6-Methyldeoxy guanosine; DNA adduct is a purine nucleoside analog. 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].
Rezatapopt is an antineoplastic agent, used to inhibit solid tumor with p53 mutation[1].
Flomoxef is a oxacephem group antibiotic, with excellent activity against various Gram-positive bacteria[1][2].
4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases[1].
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells[1].
Rhuscholide A is a benzofuran lactone that shows significant anti-HIV-1 activity, with an EC50 of 1.62 μM[1].
3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside derivative.