Bromo-PEG5-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 3.801 μM, and >10 μM, respectively.
Prolactin-Releasing Peptide (12-31), bovine is a peptide fragment of prolactin-releasing peptide (PrRP). PrRP is RF-amide peptides expressed in brain areas involved inpain modulation. Prolactin-Releasing Peptide (12-31), bovine can be used for the research of nervous system disease[1].
Hydrocortisone phosphate is the pharmaceutical term for cortisol, which is a steroid hormone, in the glucocorticoid class of hormones, increases blood sugar through gluconeogenesis, to suppress the immune system, and to aid in the metabolism of fat, protein, and carbohydrate.
Direct Red 80 (Sirius Red) is a polyazo dye used principally in staining methods for collagen and amyloid. Direct Red 80 does not release benzidine upon degradation and is safer than many traditional direct dyes[1].
N,N-dimethyl-N-((phenyl-dd5)methyl)tetradecan-1-aminium bromide is the deuterium labeled N,N-dimethyl-N-((phenyl-d5)methyl)tetradecan-1-aminium bromide[1].
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.[2].
c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively[1].
R-87366 is a water-soluble human immunodeficiency virus (HIV) protease inhibitor. R-87366 has potent inhibitory for HIV protease with a Ki value of 11 nM. R-87366 can be used for the research of anti-human immunodeficiency virus (HIV)[1].
Phenanthrene is a polycyclic aromatic hydrocarbon (PAH) and has been frequently used as an indicator for monitoring PAH contaminated matrices[1]. Phenanthrene induces oxidative stress and inflammation[2].
CL-82198 is a selective inhibitor of MMP-13.In vitro: In the presence of 10 and 20 μM of the specific MMP-13 inhibitor, CL-82198, migration of the LS174 cells was significantly reduced by 55 and 52%, respectively. . CL-82198 binds to the S1' pocket of MMP-13 leading to 89% enzyme inhibition at a concentration of 10 μg/ml. The addition of the specific MMP-13 inhibitor CL-82198 at a concentration of 10 μM resulted in a 45±5.6% reduction in the migration of LS174 cells.
COX-2-IN-21 (Compound 5c) is a selective and orally active COX-2 inhibitor with an IC50 of 0.039 μM. COX-2-IN-21 shows promising anti-inflammatory potential[1].
MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL)[1].
Schisandrin A inhibits CYP3A activity with an IC50 of 6.60 μM and Ki of 5.83 μM, respectively.
Bis-(N,N'-carboxyl-PEG4)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Homologous recombination-IN-1 is a novel RAD51-BRCA2 protein-protein interaction inhibitor (EC50=19 μM). Homologous recombination-IN-1 can interfere with homologous recombination[1].
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research[1].
H-DL-Glu(Ome)-OMe.HCl is a glutamic acid derivative[1].
N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
α-2,3-sialyltransferase-IN-1 is a noncompetitive α-2,3-sialyltransferase inhibitor with an IC50 of 6 μM.
BRD7116 competitively binds to bacterial DNA gyrase, exhibits an EC50 of 200 nM for LSCe cells, with cell-non-autonomous anti-leukemia activity.IC50 value: 200 nM (EC50, for LSCe cells)Target: DNA gyraseBRD7116 is a bis-aryl sulfone, shows evidence of stroma-mediated anti-LSCe activity. BRD7116 exhibits an EC50 of 200 nM for LSCe cells in co-culture, whereas it displays limited activity against normal HSPCs and AML cell lines (~50% inhibition at 20 μM). BRD7116 also shows activity against patient-derived, primary human leukemia cells. [1] BRD7116 inhibits LSCs via non-cell-autonomous effects on stromal cells as well as cell-autonomous induction of myeloid differentiation genes in LSCs.
RIPK1-IN-7 is a potent and selective receptor-interacting protein kinase 1 (RIPK1) inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model[1].
2-Fluoroadenine is a toxic purine bases. 2-Fluoroadenine has toxicity in nonproliferating and proliferating tumor cells. 2-Fluoroadenine can be used for researching anticancer[1].
Unifiram (DM232) is acts as a potent cognition enhancer through the activation of the AMPA-mediated neurotransmission system. Unifiram (DM232) has the potential for amnesia prevention and neurodegenerative disorder research[1][2].
DDAO is a promising near-infrared (NIR) red fluorescent probe with tunable excitation wavelength (600-650 nm) and long emission wavelength (λem = 656 nm). DDAO can de desiged for detection of the activities of different enzymes such as β-galactosidase, sulfatase, protein phosphatase 2A, carboxylesterase 2, human albumin and esterases[1].
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1].
5-Benzyloxygramine is a N protein PPI orthosteric stabilizer that exhibits both antiviral and N-NTD protein-stabilizing activities[1].
Anti-inflammatory agent 54 (compound 9c) is a derivative of Coixol and has anti-inflammatory activity. Anti-inflammatory agent 54 inhibits the NF-κB pathway and downregulates the expression of iNOS, TNF-α, IL-6 and IL-1β. Anti-inflammatory agent 54 inhibits LPS-induced nitric oxide (NO) production in RAW264.7 macrophages (IC50: 2.4 μM) and exerts in vivo anti-inflammatory activity in a mouse auricular edema model[1].
A novel potent and selective agonist of GPR84 that induces calcium response with EC50 of 0.213 uM; does not evoke calcium responses in HEK293 cells expressing other FFARs, including GPR40, GPR41, GPR119, and GPR120; increases in intracellular calcium concentrations in HEK293/Gα16/GPR84 cells with EC50 of 1.01 uM; activates several GPR84-mediated signaling pathways, including calcium mobilization, inhibition of cAMP accumulation, phosphorylation of ERK1/2, receptor desensitization and internalization, and receptor-β-arrestin interaction; reduces forskolin-stimulated cAMP accumulation in HEK293 cells with EC50 of 0.134 uM.