TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 7 μM[1].
2’-Deoxy-2’-fluoro-β-D-arabino-2-thiouridine 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].
CER8-d9 is deuterium labeled CER8.
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling[1][2].
VPC01091.4 (VPC4) is a?TRPM7?inhibitor and blocks TRPM7 current at low micromolar concentrations. VPC01091.4 is an efficacious?anti-inflammatory?agent that arrests systemic inflammation in vivo[1].
NerveGreen C3 is a cationic styrene based fluorescent dye. NerveGreen C3 can be used to track synaptic activity at neuromuscular junctions or synapses[1].
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guinea pig brain) with Ki of 0.45 μM.
Eledoisin is a specific agonist of NK2 and NK3 receptors. Sequence: {Glp}-Pro-Ser-Lys-Asp-Ala-Phe-Ile-Gly-Leu-Met-NH2.
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε)[1][2].
A-437203 is a selective D3 receptor antagonist with Ki of 71, 1.6, and 6220 nM for D2, D3, and D4 receptors, respectively.
HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38)[1].
Globomycin is a lipopeptide antibiotic and a signal peptidase II (LspA) inhibitor. Globomycin inhibits processing of the prolipoprotein by binding irreversibly to the peptidase. Globomycin has toxic for the mollicute Spiroplasma melliferum with a MIC in the range 6.25-12.5 μM[1][2].
Z-Glu(OBzl)-OH is a glutamic acid derivative[1].
(3S,4aS,10aS)-3-(Acetyloxy)-2,3,4,4a,10,10a-hexahydro-6-hydroxy-1,1,4a-trimethyl-7-(1-methylethyl)-9(1H)-phenanthrenone (compound 3), a Palmitate, can be isolated from the root tissue of Salvia miltiorrhiza. (3S,4aS,10aS)-3-(Acetyloxy)-2,3,4,4a,10,10a-hexahydro-6-hydroxy-1,1,4a-trimethyl-7-(1-methylethyl)-9(1H)-phenanthrenone (compound 3) shows anti-cancer activity against human cancer cell lines with DC50s of 25.5 μg/mL (HeLa), 37.5 μg/mL (HepG2), 30.2 μg/mL (OVCAR-3), respectively[1].
D-Cycloserine is an analog of the amino acid D-alanine.Target: AntibacterialD-Cycloserine selectively potentiated the duration of motor cortical excitability enhancements induced by anodal tDCS. D-Cycloserine alone did not modulate excitability [1]. Participants receiving d-cycloserine in addition to exposure therapy reported significantly less social anxiety compared with patients receiving exposure therapy plus placebo. Controlled effect sizes were in the medium to large range [2]. Chronic D-cycloserine significantly reduced nicotine self-administration selectively in rats with low baseline nicotine use, but was ineffective with the rats with higher levels of baseline nicotine self-administration [3].
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile[1].
Kadsurenin A is a bioactive Lignan from the genus Piper L.
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion[1][2].
BIO-1211 is a high selective α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively[1][2][3].
Methyl 3-aminopropanoate hydrochloride is prepared by esterification of Β-Alanine (I). Methyl 3-aminopropanoate hydrochloride can be used in the synthesis of bidentate pyridine-acid ligand[1].
CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities[1].
Photosensitizer-1 is a photosensitizer.
(E)-Ajoene is a oxygenated ajoene and organosulfur compound, which can be acquired via allicin decomposing. The polysulfides from garlic can be converted by human red blood cells into hydrogen sulfide (H2S) and allyl glutathione. (E)-Ajoene has been proved to show neuroprotective effects against ischemic damage. (E)-Ajoene is orally active to inhibit lipid peroxidation. (E)-Ajoene increases the number of cresyl violet-positive neurons and decreases the number of reactive gliosis in the CA1 region[1][2].
AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
PKCδ Peptide Substrate is an absolutely specific substrate for the δ-type of PKC, with a sequence corresponding to sequence 422-443 of murine eEF-1α and containing Thr-431[1].
Varokibart (TEV-53275) is a human IgG4λ antibody targeting IL5[1].
RAF709 is a potent, selective, and efficacious RAF inhibitor with IC50s of 0.4 nM and 0.5 nM for BRAF and CRAF, respectively[1]. Antitumor efficacy[1].
1-Iodobenzene-d2 is the deuterium labeled 1-Iodobenzene[1].
Camobucol is an orally active, phenolic antioxidant and anti-inflammatory compound with antirheumatic properties.
TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.