ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination treatment with docetaxel[1].
Oxaliplatin is a DNA synthesis inhibitor. It causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death.
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation[1][2][3][4].
[Tyr8,Nle11] Substance P is a Substance P (HY-P0201) analog. Substance P is a peptide mainly secreted by neurons and is involved in many biological processes, including nociception and inflammation[1].
Gantenerumab is a fully human anti-amyloid-β (Aβ) IgG1 monoclonal antibody demonstrates sustained cerebral amyloid-β binding. Gantenerumab can be used for Alzheimer's disease research[1].
Tau Peptide (255-314) (Repeat 2 Domain) (human) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development[1].
Ciprofloxacin (Bay-09867) lactate is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin lactate induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin lactate has anti-proliferative activity and induces apoptosis. Ciprofloxacin lactate is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity[1][2][3][4].
Clopidogrel-d3 (hydrochloride) is the deuterium labeled Clopidogrel hydrochloride[1].
Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.IC50 Value: 3.8 nM [1]Target: proteasomein vitro: CEP-18770 and bortezomib showed comparable potency against chymotrypsin-like proteasome activity, cellular inhibitory activity (IC50) values of 3.8 (± 1.0) nM and 3.8 (± 0.4) nM, respectively, CEP-18770 had a 2- to 11-fold lower cytotoxic potency compared with bortezomib against solid tumor cell lines, comparable potency against 2 hematologic tumor cell lines, and a similar spectrum of antiproliferative activity with IC50 values for both compounds of less than 35 nM [1].in vivo: in MM xenograft models, the addition of CEP-18770 IV to melphalan completely prevented the growth of both melphalan-sensitive and melphalan-resistant tumours. The combination of CEP-18770 IV and bortezomib induced complete regression of bortezomib-sensitive tumours and markedly delayed progression of bortezomib-resistant tumours compared to treatment with either agent alone [2]. Age matched MRL/lpr or NZBWF1 mice with established SLE or LN, respectively, were treated with delanzomib either 3 mg/kg once or twice weekly intravenously or orally at 10 mg/kg [3]. Toxicity: CEP-18770 showed a favourable safety profile with lack of neurotoxicity and linear plasma PK. The definition of the optimal biological dose and schedule of treatment is actively pursued because of the high incidence of skin toxicity of the twice a week schedule [4].Clinical trial: CEP-18770 in Combination With Lenalidomide and Dexamethasone in Relapsed or Refractory Multiple Myeloma. Phase1/2
SDZ 220-581 Hcl is a potent, competitive antagonist at the NMDA glutamate receptor subtype(pKi= 7.7).IC50 Value: Target: NMDA receptorin vitro: Wake-promoting doses of LSN2463359 and LSN2814617 attenuated deficits in performance induced by the competitiveNMDA receptor antagonist SDZ 220,581 in two tests of operant behaviour: the variable interval 30 s task and the DMTP task [1].in vivo: Administration of SDZ 220-581 or CGS 19755 was associated with a robust reduction in PPI, whereas L-701,324, 4-Cl-KYN or MLA failed to alter PPI [2]. With the most active agent, SDZ 220-581, full protection against maximal electroshock seizures (MES) was obtained at oral doses of 10 mg/kg in rats and in mice. The compound had a fast onset (< or = 1 hr) and a long duration (> or = 24 hr) of action [3]. Rats were pretreated with clozapine (0 or 5.0 mg/kg) or haloperidol (0 or 0.1 mg/kg), together with SDZ 220-581 (0 or 2.5 mg/kg), and tested. SDZ 220-581 and SDZ EAB-515 decreased PPI without affecting startle magnitude [4].
LSTc (LS-tetrasaccharide c) is a human lactooligosaccharide presents on glycoproteins and glycolipids. LSTc is also a specific human JC polyomavirus (JCV) recognition motif. LSTc has good potential for the study of progressive multifocal leukoencephalopathy (PML)[1].
RKLLW-NH2 is a Cathepsin L inhibitor[1].
FA-Leu-Gly-Pro-Ala-OH is a substrate of microbial collagenase[1].
ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'[1].
2-Chloro-5-cyanopyridine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
4-Butylaniline-d9 is the deuterium labeled 4-Butylaniline[1].
Apigenin 7-O-sophoroside is a flavonoid glycoside isolated from Lonicera gracilipes var. glandulosa[1].
ATR-IN-5 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-5 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent CN112047938A, compound D24)[1].
Cyclobenzaprine-d6 (hydrochloride) is deuterium labeled Cyclobenzaprine (hydrochloride).
Cyclopropyl-2,2,3,3-amine-d4 is the deuterium labeled Cyclopropanamine[1].
CM037 is a selective inhibitor of ALDH1A1 (aldehyde dehydrogenase 1A1) with an IC50 of 4.6 µM[1].
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCH1) antagonist with antidepressant-like activity, it differentiates from classic anxiolytic and antidepressant drugs.SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.SNAP 94847 is a high affinity antagonist (pA2 = 7.81) of MCH-evoked inositol phosphate formation[1].
Lindenenol is isolated from Radix linderae, with antioxidant and antibacterial activities[1].
Virstatin inhibits the pili system synthesis and prevents A. baumannii biofilm formation. Virstatin also inhibits dimerization of the transcriptional activator ToxT[1][2].
NSC689857 is a potent EGFR and SCFSKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others[1][2].
Sanfetrinem (GV104326) sodium is a beta-lactamase-stable antibiotic. Sanfetrinem sodium has broad-spectrum activity against gram-positive and gram-negative bacteria[1].
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer[1].
trans-Permethrin is a transconfiguration of Permethrin (HY-B0887). Permethrin is an insecticide and neurotoxin[1].
Sec61-IN-2 (A347) is a protein secretion inhibitor (extracted from patent WO2020176863)[1].
Humanin C8A-HN is a biological active peptide. (Protection activity of humanin (HN) against neuronal cell death is abrogated in this peptide, where Cys8 is substituted by Ala.)