Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models[1][2].
Glyurallin A (Compound 79) is isolated from the naturalGlycyrrhiza uralensis. Glyurallin A inhibitsα-Glucosidase(HY-P2802)(IC50=0.3 μM). Glyurallin A can be used in the study of anti-diabetes[1].
Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. IC50 value: 0.22 uM [1]Target: Flt3; PDGFRβ; c-Kitin vitro: Tandutinib has little activity against EGFR, FGFR, KDR, InsR, Src, Abl, PKC, PKA and MAPKs. Tandutinib inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC50 of 10-100 nM. Tandutinib also inhibits the proliferation of human leukemia Ba/F3 cells containing FLT3-ITD mutations with IC50 values of 10-30 nM, and the FLT3-ITD-positive Molm-13 and Molm-14 cells with an IC50 of 10 nM. In FLT3-ITD-positive Molm-14 cells but not the FLT3-ITD-negative THP-1 cells, Tandutinib treatment leads to significant apoptosis by 51% and 78% at 24 and 96 hours, respectively, due to specific FLT3 inhibition [1]. Tandutinib preferentially inhibits the growth of blast colonies from FLT3 ITD-positive compared with ITD-negative patients with AML, without affecting colony formation by normal human progenitor cells [2].in vivo: Oral administration of Tandutinib at 60 mg/kg bid significantly increases the survival in mice bearing Ba/F3 cells expressing W51 FLT3-ITD mutant, and gives a significant reduction in mortality in a mouse bone marrow transplantation model [1]. Tandutinib treatment at 180 mg/kg twice daily has mild toxicity toward normal hematopoiesis, however, it is a dose at which Tandutinib is effective in treating FLT3 ITD-positive leukemia in mice [2].
L-733060 hydrochloride is a potent tachykinin NK1 receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent[1][2].
Reozalimab is a bispecific antibody targeting to PD-1/PD-L1. Reozalimab mediates antibody-dependent cell cytotoxicity in cancer research[1][2].
JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents[1].
Imexon is an iminopyrrolidone aziridine with anti-cancer activity.
2'-O-MOE-U is an oligonucleotide, can be used for oligonucleotide synthesis[1].
3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis[1].
4-Bromo-3-hydroxybenzoic acid is a metabolite of Brocresine and a histidine decarboxylase (HDC) inhibitor with IC50s of 1 mM for both rat fetal and rat gastric HDC. 4-Bromo-3-hydroxybenzoic acid also inhibits aromatic-L-amino acid decarboxylase from hog kidney and rat gastric mucosa in vitro with IC50s of 1 mM for both enzymes[1][2].
Olanzapine(LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.IC50 Value:Target: 5-HT ReceptorOlanzapine is a thienobenzodiazepine that blocks especially the serontonin (5-hydroxytryptamine [5-HT]) 5-HT2A and the dopamine D2 receptors (Ki values are 4 and 11 nM respectively) as well as muscarinic (M1), histamine (H1), 5-HT2C, 5-HT3 to 5-HT6, adrenergic (α(l)), and D4 receptors. Atypical antipsychotic for the treatment of schizophrenia. Olanzapine displays anticholinergic properties.
Glyoxalase I inhibitor 7 (Compound 6) is a glyoxalase I (Glo-I) inhibitor with an IC50 of 3.65 μM. Glyoxalase I inhibitor 7 can be used as anticancer agent[1].
3,4,5-Trimethoxybenzaldehyde is an intermediate for the synthesis of various pharmaceuticals, especially for trimethoprim used to treat bacterial infections, including urinary tract pathogens infection[1].
CAY 10434 dihydrochloride is a potent CYP4A hydroxylase inhibitor. CAY 10434 dihydrochloride improves contractile response to angiotensin II with the maximal contractile response (Emax) 6764 mg[1].
Prim-O-glucosylcimifugin exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by through regulating JAK2/STAT3 signaling.
Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
Ro 22-9194 inhibits aggregation and thromboxane Az (TXA2) synthetase activity in rabbit and human platelets. Ro 22-9194 has a potent inhibitory action against various types of model arrhythmias. Ro 22-9194 has non-cholinergic cardiac depressant properties with its vasodilating action[1][2].
Antibacterial agent 33, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Zeteletinib (BOS-172738) shows selective inhibitory activity against RET, PDGFR, KIT, NTRK and FLT3 kinases. Zeteletinib has antitumor activity[1].
Valpromide is an amide derivative of valproic acid and inhibits human epoxide hydrolase.
SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
TPI-1 is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM.
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].
Lactoferricin, bovine is an iron-binding glycoprotein derived from the acidic hydrolysis of bovine lactoferrin. Lactoferricin, bovine has bactericidal, antifungal, antiparasitic, antitumor, antiviral, and immunomodulatory activities[1].
(-)-15-Deoxyspergualin is a potent antitumor agent. (-)-15-Deoxyspergualin shows strong inhibition against mouse leukemia L-1210[1].
PF-06454589 is a potent and selective LRRK2 inhibitor.
Imisopasem manganese (M40403) is a stable non-peptidyl mimetic of manganese superoxide MnSOD.
Pronethalol-d6 ((±)-Pronethalo-d6) is the deuterium labeled Pronethalol. Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs)[1][2][3].
Benzylideneacetone is an endogenous metabolite.
TO-PRO-3 (iodide) is a highly efficient blue fluorescent dye that can stain cytoplasm as a cell tracer.