7-Hydroxyquetiapine (ICI 214227) is the major active metabolite of antipsychotic medicine Quetiapine[1].
LNnDFH I is a natural product that can be isolated from human urine[1].
UC2288 is a novel, cell-permeable, and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM[1].
A potent, selective peptide inhibitor of hERG channel with IC50 of 3.3 nM for hERG1 channels; displays no effect at 100 nM on hEAG, hSK1, rSK2, hIK, hBK, KCNQ1/KCNE1, KCNQ2/KCNQ3, KCNQ4 channels, and minimal effect on rELK1; prolongs QTc intervals significantly and concentration-dependently (4.7 and 16.3% at 10 and 100 nM, respectively).
Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells[1].
7-Oxodehydroabietic acidis a diterpene resin acid isolated from the roots of the pine Pinus densiflora. 7-Oxodehydroabietic acid play a defensive role against herbivorous insects via insect endocrine-disrupting activity[1].
H-Glu(OMe)-OH is a glutamic acid derivative[1].
Azetidin-3-ol hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azetidin-3-ol hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthes PROTAC.
Ac-rC Phosphoramidite is used for the oligoribonucleotide phosphorodithioate modification (PS2-RNA)[1].
MIF098 is a macrophage migration inhibitory factor (MIF) antagonist. MIF098 inhibits proliferation, migration and fibrosis of pulmonary smooth muscle cells. MIF098 can be used for immunoinflammation-related disease research[1].
LysoTracker Yellow HCK 123 is a potent yellow membrane-permeable fluorescent probe. LysoTracker Yellow HCK 123 is a weakly basic amine that selectively accumulates in cellular compartments with low luminal pH. (λex=465 nm, λem=535 nm)[1].
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation.
123C4 is a potent, selective and competitive agonist of the receptor tyrosine kinase EPHA4, with a Ki value of 0.65 μM[1].
KDM2B-IN-3 is a histone demethylase KDM2B inhibitor extracted from patent WO2016112284A1, compound 183c. KDM2B-IN-3 can be used for the research of cancer[1].
SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases[1].
ST1074 is a dual CerS2/CerS4 inhibitor that induces apoptosis. ST1074 can be used in cancer research[1].
CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM.
N4-Desmethyl wyosine 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].
1-Octanol-d2 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
IMD-0354 is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC 50 of 1.2±0.3 uM.
SBE13 is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 poorly inhibits Plk2 (IC50>66 μM) or Plk3 (IC50=875 nM).
MC-Val-Cit-PAB is a cathepsin cleavable ADC linker that is used for making antibody-drug conjugate. FDA approved drugs such as brentuximab vedotin use this linker.
16-Oxoalisol A is a triterpene in Rhizoma Alismatis. Rhizoma Alismatis is a commonly used traditional Chinese medicine (TCM). Rhizoma Alismatis can be used for the research of urinary tract diseases[1].
3,4,9,10-Perylenetetracarboxylic-diimide (PTCDI), an organic heteropolycyclic compound, is a dimethylimine that can be used in biological dyes and indicators[1].
Boc-NH-PEG7-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Lithospermoside (Griffonin) is a nature product isolated from the stem bark of Ochna schweinfurthiana F. Hoffm[1].
Biotin-PEG7-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties[1].
α-Conotoxin Im-I is a selective α7/α9 nAChR antagonist, blocking α7 nicotinic receptors with the highest apparent affinity, while having an 8-fold lower affinity for homomeric α9 nicotinic receptors. α-Conotoxin Im-I is toxic and induces seizures in rodents. α-Conotoxin Im-I is a tool for studying neuronal nAChR[1][2].
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.