Edecesertib (GS-5718) is a selective, potent, orally active IRAK-4 inhibitor. Edecesertib has anti-inflammatory activity. Edecesertib can be used for rheumatoid arthritis (RA) and lupus erythematosus (LE) research[1][2].
ATIC-IN-1(compound 14) is an inhibitor targeting to Aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC) dimerization with a Ki value of 685 nM. ATIC dimerization is crucial for its aminoimidazole carboxamide ribonucleotide (AICAR) transformylase activity. ATIC-IN-1 exhibits anti-tumor activity via reduction in cell numbers and cell division rates[1].
MQAE is a fluorescent indicator that is quenched via collision with chloride, and is more sensitive and selective than 36Cl and microelectrode-based methods for chloride measurement in cells.
C-176 is a strong and covalent mouse STING inhibitor.
Suc-Gly-Pro-AMC is a fibroblast activation protein (FAP)-specific substrate. Suc-Gly-Pro-AMC can be used to study the activity of FAP[1].
Panaxydiol exhibits histamine-release inhibition activity[1].
DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models[1].
N-(tert-Butoxycarbonyl)-O-(tert-butyl)-L-threonyl-L-proline is a proline derivative[1].
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity[1].
eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-2 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 1188)[1].
Fmoc-Tyr(Me)-OH is a tyrosine derivative[1].
Dunnione (CompoundⅠ) is a pigment. Dunnione can be isolated from the leaves of Didymocarpus pedicellata[1].
Tos-PEG8-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Indoprofen is a non-steroidal anti-inflammatory drug, provide insight into treatments for spinal muscular atrophies.
2’-Deoxy-O6-[2-(4-nitrophenylethyl)]guanosine 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].
Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors[1][2].
Dansyl-Gly-Cys-Val-Leu-Ser is a dansyl-labeled peptide[1].
Heptaethylene glycol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
D-Phenylalanine, N-[N-[(1,1-dimethylethoxy)carbonyl]-L-leucyl]-, phenylmethyl ester is a phenylalanine derivative[1].
1-Myristoyl-2-myristoyl-sn-glycero-3-phosphocholine-d27 is deuterium labeled 1-Myristoyl-2-myristoyl-sn-glycero-3-phosphocholine.
Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. Target: Histamine H1-receptorMizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors. Side effects can include dry mouth and throat.Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials have shown mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with chronic idiopathic urticaria. Available data also suggest that prophylactic administration of mizolastine is significantly more effective than placebo and as effective as prophylactic terfenadine in delaying the onset of symptoms of seasonal allergic rhinitis.
TLR7/8-IN-1 is a crystalline from of a TLR7/TLR8 inhibitor extracted from patent WO2019220390, compound 2b. TLR7/8-IN-1 can be used for the research of autoimmune disease[1].
BMS-193885 is a potent, selective, competitive, and brain penetrant neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM, and has an IC50 of 5.9 nM for hY1, which displays > 100, > 160, > 160 and > 160-fold selectivity over α1, hY2, hY4 and hY5 receptors, respectively [1] [2].
2-hydroxychalcone, a natural flavonoid, is a potent antioxidant, inhibiting lipid peroxidation. 2-Hydroxychalcone induces apoptosis by Bcl-2 downregulation. 2-Hydroxychalcone inhibits the activation of NF-kB[1][2][3].
cRIPGBM(chloride), an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models[1].
COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.
H-Gly-Gly-Lys-OH is a biologically active peptide.
Isoliquiritin, isolated from Licorice Root, inhibits angiogenesis and tube formation. Isoliquiritin also exhibits antidepressant-like effects and antifungal activity[1][2][3].
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70[1][2].