Palifosfamide (tromethamine) is a synthetic alkylating agent with potential antineoplastic activity. As the stabilized active metabolite of ifosfamide, palifosfamide (tromethamine) irreversibly alkylates and crosslinks DNA through GC base pairs. This leads to an inhibition of DNA replication and ultimately cell death. Compared to ifosfamide, palifosfamide (tromethamine) is less toxic.
Rac-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM[1].
m-PEG24-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pectin is a heteropolysaccharide, derived from the cell wall of higher plants. Pectin involves in the formation of nanoparticles as a delivery vehicle of drugs. Pectin is also an adsorbent, a broad-spectrum antimicrobial agent that binds to bacteria toxins and other irritants in the intestinal mucosa, relieves irritated mucosa[1][2][3].
Piperonyl acetone is a food additives[1].
ROCK-IN-D2 is an effective and selective inhibitor of ROCK.
Isosativenediol is a sesquiterpene compound. Isosativenediol can be purified from Cochliobolus sativus, an endophytic fungus isolated from the desert plant Artemisia Desertorum[1][2].
Bis-Biotin-PEG23 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
8-Geranyloxy-5,7-dimethoxycoumarin is a natural geranyloxycoumarin compound[1].
6"-O-Acetylisoquercitrin is a natural product that can be found in Lingonberry[1].
GPR40 Activator 2 is a potent GPR40 activator from patents WO 2012147516 A1, WO 2012046869A1 and WO 2011078371 A1.
Sotiburafusp alfa is a bispecific fusion protein, which is a humanized VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) fused via the peptide linker 101GGSGGSGGSGGSGGS115 to the N-terminus of the heavy chain (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain variant L352>A, L353>A. Sotiburafusp alfa is also an angiogenesis inhibitor[1].
Spexin-2 (53-70), human,mouse,rat (NPQ 53-70) is a biological active peptide. (This is Spexin-2 (53-70), non-amidated version of the novel peptide hormone that is derived from prohormone proNPQ and is conserved amongst mammalian species. It is a central modulator of cardiovascular and renal function. Spexin-2, when administered to rats, decreases heart rate and increases urine flow rate)
WAY-323756 is an active molecule for research into amyloid diseases and synucleinopathies.
3,6-Dihydroxyflavone is an anti-cancer agent. 3,6-Dihydroxyflavone dose- and time-dependently decreases cell viability and induces apoptosis by activating caspase cascade, cleaving poly (ADP-ribose) polymerase (PARP). 3,6-Dihydroxyflavone increases intracellular oxidative stress and lipid peroxidation[1].
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition[1].
K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRASG12C[1].
4',6,7-Trimethoxyisoflavone is an isoflavone with antimicrobial activities against a wide range of bacteria and fungi. 4',6,7-Trimethoxyisoflavone also has antioxidant effects[1].
Octakis-(6-bromo-6-deoxy)-γ-cyclodextrin is a perbrominated γ-cyclodextrin at the primary side. Octakis-(6-bromo-6-deoxy)-γ-cyclodextrin is also a commonly used intermediate in the modification of cyclodextrin[1].
PI3KC2α-IN-3 is a potent and highly selective PI3KC2α inhibitor (IC50: 126 nM). PI3KC2α-IN-3 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-3 impairs endocytic membrane dynamics and membrane remodeling. PI3KC2α-IN-3 can be used in the research of thrombosis, diabetes and cancers[1].
Cyclophosphamide-d8 is deuterium labeled Cyclophosphamide. Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifoliaWILLD, with anti-stress effect, prolonging the sleeping time in animals[1][2]. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits[2].
hMAO-B-IN-3 (Compound 15) is a potent inhibitor of hMAO-B with an IC50 of 47.4 nM. hMAO-B-IN-3 is playing favourable drug-like properties and a broad safety window. hMAO-B-IN-3 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands[1].
L-carnitine hydrochloride ((S)-Carnitine Hydrochloride) has been used to study sulfur factor transporter SLC22A4 and carnitine transporter slc22a5 in ergot. L-Carnitine hydrochloride is also used to get palmitic acid into mitochondria[1][2].
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs[1].
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases[1].
(Rac)-Efavirenz-d4 ((Rac)-DMP 266-d4) is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumour activity[1].
(R)-Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. (R)-Preclamol inhibits the locomotor activity of mice and rats in low doses[1].
Itolizumab (Anti-Human CD6 Recombinant Antibody) is a humanized recombinant anti-CD6 monoclonal antibody (MAb) targeting the extracellular SRCR distal domain 1 of CD6. Itolizumab reduces T-cell proliferation and inhibits the production of pro-inflammatory cytokines, such as INF-γ, TNFα and IL-6. Itolizumab can be used in the research of psoriasis, rheumatoid arthritis (RA), COVID-19[1][2][3].