Momelotinib-d10 (CYT387-d10) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally active and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
N-(m-PEG4)-N'-(Acid-PEG3)-benzothiazole Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
TAK-901-d3 is the deuterium labeled TAK-901. TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively[1][2].
BMS-309403 is a potent, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM.
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia[1][2].
CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors[1].
Carbon-13C is the 13C labeled Carbon[1].
CKS-17 is a synthetic retroviral envelope peptide. CKS-17 has the highly conserved amino acid sequences occurring within the transmembrane envelope protein of many animal and human retroviruses. CKS-17 acts as an immunomodulatory epitope and exhibits suppressive properties for numerous immune functions[1][2][3].
Complanatoside B is a P. chinense Fisch flavonoid with potential anti-inflammatory effects[1].
PF-07258669 is a melanocortin-4 receptor (MC4) antagonist. PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa[1].
BT-11 is an orally available LANCL2 binding compound for treating inflammatory bowel disease.
Cyclosporin U (SMP0V32C6L) is an cytostatic agent that plays an important role in preventing rejection of transplanted organs[1].
Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline, which is an irreversible inhibitor of monoamine oxidase.
OUL232 is a potent inhibitor of mono-ARTs PARP7, PARP10, PARP11, PARP12, PARP14, and PARP15. OUL232 is the most potent PARP10 inhibitor described to date (IC50=7.8 nM), as well as the first PARP12 inhibitor ever reported[1].
Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM[1][2].
UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies. Target: L3MBTL3The low anticipated affinity of UNC1079 was confirmed, as it demonstrated an activity versus L3MBTL3 of > 10 μM by AlphaScreen, which is >1000-fold weaker than UNC1215. UNC1079 also displays weak binding by ITC.
Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM.
Tetraphenylporphyrin (TPP;Tetraphenylporphine;meso-Tetraphenylporphyrin) is a symmetrically substituted porphyrin-based heterocyclic compound and used as a structural block for supramolecular synthesis. Tetraphenylporphyrin derivatives can be used for cancer research[1].
Fmoc-D-Nle-OH is a leucine derivative[1].
PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity[1].
N3-L-Dap(Boc)-OH is a click chemistry reagent containing an azide group. Click chemistry is a powerful chemical reaction with excellent bioorthogonality features: biocompatible, rapid and highly specific in biological environments[1].
Plocabulin (PM060184) is a novel tubulin-binding agent binding to αβ-tubulin dimer with nanomolar affinity, inhibits a panel of 23 tumor cell lines with GI50 of 20 pM-5 nM; inhibits angiogenesis by modulation of microtubule dynamics in endothelial cells; also shows antifungal activity virtually abolishing growth of the filamentous fungus Aspergillus nidulans.
PSB11 hydrochloride is an antagonist with reverse excitatory activity for human A3 Adenosine Receptor with high affinity (Ki=2.3 nM)[1].
Ganoderic acid R is a potent anticancer agent. Ganoderic acid R inhibits the growth by inducing apoptosis on tumor cell line. Ganoderic acid R possesses significant cytotoxicity on a multidrug resistance (MDR) tumor cell line (KB-A-1/Dox) and a sensitive tumor cell line (KB-A-1)[1].
Lenalidomide-4-OH is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-OH can be connected to the ligand for protein by a linker to form PROTAC.
AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate also inhibits the DNA polymerase of HBV. AZT triphosphate activates the mitochondria-mediated apoptosis pathway[1][2][3].
FL118-14-Propanol is a FL118 derivative. FL118-14-Propanol synthesized ADC molecule has good anti-tumor effect in mice[1].
D-thyroxine (sodium) (D-T4 (sodium)) is a laevorotatory isomer of thyroxine, and can used for the research of the dysfunctions of thyroid[1][2].
1,2-Distearoyl-sn-glycero-3-phosphorylcholine-d83 is deuterium labeled 1,2-Distearoyl-sn-glycero-3-phosphorylcholine. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine (1,2-Distearoyl-sn-glycero-3-PC; DSPC) is a cylindrical-shaped lipid. 1,2-Distearoyl-sn-glycero-3-phosphorylcholine is used to synthesize liposomes, and is the lipid component in the lipid nanoparticle (LNP) system[1][2].