Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.
MRE-269-d6 is deuterium labeled MRE-269. MRE-269 is an active metabolite of selexipag, and acts as a selective IP receptor agonist.
Propargyl-PEG8-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis.
4-Thio-2’-deoxyuridine is a purine nucleoside analog. 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].
Cenegermin is a recombinant human nerve growth factor (rhNGF). Cenegermin can be used in the research of neurotrophic keratitis[1].
(22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid (compound 15) is an antitubercular agent with MIC value of 12.5 μg/mL for Mycobacterium tuberculosis H37Ra. (22S,24E)-3β,22-Diacetoxylanosta-7,9(11),24-trien-26-oic acid shows cytotoxicity with IC50 value of 32 μM for Vero cells[1].
Adamantane-d16 is the deuterium labeled DL-Histidine[1].
Alemtuzumab (Campath-IH) is a humanized monoclonal antibody against CD52, a glycoprotein expressed on the surface of most lymphoid, and to a lesser extent, myeloid cell types. Alemtuzumab selectively targets the CD52 antigen to induce profound lymphocyte depletion, followed by recovery of T and B cells with regulatory phenotypes[1][2].
Basic green 4 (Malachite green) is a cationic dye. Basic green 4 also is an N-methylated diaminotriphenylmethane dye to be used for coloring purpose[1].
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity[1]. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function[2].
Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
FATP1-IN-1 is a fatty acid transport protein 1 (FATP1) inhibitor. FATP1-IN-1 is an inhibition of recombinant human or mouse acyl-CoA synthetase activity of FATP1, with the IC50 values of 0.046 μM or 0.60 μM, respectively[1].
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations[1].
Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over allproteases tested (IC50 > 67 μM).IC50 value: 1.6 nM [1]Target: DPP-4 inhibitorin vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays. in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction).
(+)-7'-Methoxylariciresinol is a lignan glucoside that can be isolated from Cyclea racemosa[1].
2-Chloro-N6-cyclopentyl 2’-deoxy- adenosine is a purine nucleoside analog. 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].
Palivizumab (MEDI 493), a humanized respiratory syncytial virus monoclonal antibody, reduces respiratory syncytial virus (RSV) infection[1].
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist[1].
(Rac)-Tavapadon ((Rac)-PF-06649751; (Rac)-CVL-751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity[1].
5-DTAF is a isomeric fluorescein derivative that directly react with polysaccharides and other alcohols in aqueous solution at pH ＞ 9. The maximum of the 5-DTAF emission profile is at a wavelength of 518 nm after excitation at 488 nm[1].
FmocNH-PEG2-CH2CONH-PEG2-CH2COOH is an optimized, extended PEG-like linker[1].
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively[1].
Pedaliin is a bioactive component obtained from the ethanol extract of Sesame (Sesamum indicum L.) leaves (SLs). Pedaliin shows in vitro antioxidant and anti-colon cancer efficacy with radical scavenging activity and ferric reducing antioxidant power (FRAP)[1][2].
UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB)[1].
Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
Liensinine Perchlorate is a constituent of Nelumbo nucifera Gaertn, with ani-hypertension and anti-cancer activities. Liensinine Perchlorate induces colorectal cancer (CRC) cell apoptosis[1].
Saccharopine (L-Saccharopine), a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine by the lysine-ketoglutarate reductase. Saccharopine is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine impairs development by disrupting mitochondrial homeostasis[1][2][3].
H-Thr-Gly-OH is a biologically active peptide.