Tos-PEG7-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM; 3-Deazaadenosine has anti-inflammatory, anti-proliferative and anti-HIV activity.
Thalidomide-NH-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties[1].Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
ABT-737 is a selective and BH3 mimetic Bcl-xL, Bcl-2 and Bcl-w inhibitor with EC50s of 78.7 nM, 30.3 nM and 197.8 nM, respectively.
T-1095 is a selective and orally active Na+-glucose cotransporter (SGLT) inhibitor with IC50s of 22.8 µM and 2.3 µM for human SGLT1 and SGLT2, respectively. T-1095 can be used for diabetes research[1].
Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3].
Emicoron is a new promising G4 ligand and bind G-rich oncogene promoters. Emicoron possesses a marked antitumoral activity? alone or in combination with chemotherapeutics in vivo. Emicoron can be used for cancer research[1].
Ubamatamab (REGN4018) is a human bispecific antibody targeted against Mucin 16 (MUC16) and CD3. Ubamatamab demonstrates potent antitumor activity[1].
KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
N-Demethylricinine is a ricinine, can be interconverted with ricinine in senescent and green castor plant leaves. Ricinine, is a α-pyridone alkaloid biosynthetically related to the pyridine nucleotide cycle. The alkaloid catabolism of ricinine is associated with aging process[1].
(S)-(+)-Imperanene can be isolated from Imperata cylindrica. Imperata cylindrica has diuretic and antiinflammatory activity[1].
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM[1].
β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells[1].
15-Keto Travoprost (15-Keto Fluprostenol isopropyl ester) is a metabolite of Travoprost (HY-B0584). 15-Keto Travoprost shows stimulatory effect on the growth and thickening of the eyelashes[1][2].
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia[1].
Licostinel (ACEA-1021) is a glycine receptor antagonist (IC50: 59 nM). Licostinel has neuroprotective activity[1][2][3].
SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
Viral polymerase-IN-1 hydrochloride, a Gemcitabine (HY-17026) derivative, potently inhibits influenza A and B viruses infection with IC90 values of 11.4-15.9 μM. Viral polymerase-IN-1 hydrochloride is active against SARS-CoV-2 infection. Viral polymerase-IN-1 hydrochloride suppresses influenza virus infection by affecting viral RNA replication/transcription in cells[1].
Endo-BCN-Nitrobenzene is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Camoteskimab (AVTX-007) is a fully human, high-affinity anti-IL-18 monoclonal antibody. Camoteskimab has the potential for the autoinflammatory diseases research, including adult-onset Still’s disease (AOSD)[1].
WZ4141 is an API intermediate.
FT011, a new anti-fibrotic and an anti-inflammatory agent, prevents glycogen accumulation by reducing glycogenin mRNA translation.In vitro: FT011 do not change glycogen synthase or glycogen phosphorylase enzyme activities but prevent both glycogenin mRNA synthesis and accumulation of Armanni-Ebstein lesions in the diabetic kidney. [1] FT011 inhibit both TGF-β1 and PDGF-BB induced collagen production as well as PDGF-BB-mediated mesangial proliferation. FT011 reduced albuminuria, glomerulosclerosis and tubulointerstitial fibrosis. [3]In vivo: The reference for FT011 is 200 mg/kg/day [1]. rats are studied for 8 and 32 weeks and receiving intravitreal injections of FT011 (50 μM). FT011 reduces etinal leukostasis, microglial density and mRNA levels of intercellular adhesion molecule-1 (ICAM-1). Late intervention with FT011 reducesacellular capillaries and the elevated mRNA levels of collagen IV and fibronectin in diabetic rats. [2]
L-Leucinamide (hydrochloride) is an amino acid derivative with anti-inflammatory properties[1].
2'-O,4'-C-Methyleneadenosine (LNA-A) is a locked nucleic acid (LNA) and is also an adenosine analog[1].
Oleanolic acid hemiphthalate disodium salt is an anti-inflammatory agent[1].
Glu(OtBu)-Val-Cit-PAB-OH (compound L5-1c) is an non-cleavable ADC linker. Glu(OtBu)-Val-Cit-PAB-OH has been used to synthesis protein-tubulysin conjugates[1].