SB 206553 is a potent and selective 5-HT2B/5-HT2C receptor antagonist with pA2 of 8.89 for rat 5-HT2B, pKi of 7.92 for human 5-HT2C, displays >80-fold selectivity over other 5-HT receptor subtypes; exhibits anxiolytic-like properties both in vitro and in vivo. Anxiety Discontinued
RBP4 inhibitor 1 (compound 43b) is a potent and orally active retinol-binding protein 4 (RBP4) inhibitor with IC50s of 28 nM and 110 nM for human and mouse RBP4. RBP4 inhibitor 1 has a potent and long-lasting blood RBP4-level-reducing effect in mice[1].
Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM)[1].
6-Aldehydoisoophiopogonone A is a homoisoflavonoid that can be isolated from Ophiopogon japonicus[1].
Azido-PEG3-O-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
E-7050 is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
Azido-PEG8-NHBoc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Aminooxy-PEG2-alcohol is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. Aminooxy-PEG2-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[2].
Amygdalin is a plant glucoside isolated from the stones of rosaceous fruits, such as apricots, peaches, almond, cherries, and plums.
PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile[1].
Methyl 1-aminocyclopropanecarboxylate hydrochloride is an alanine derivative[1].
(2S,3R)-Brassinazole, the enantiomer of Brassinazole (BRZ). Brassinazole inhibits brassinosteroid (BR) biosynthesis, via acting on the oxidative processes from 6-oxo-campestanol to teasterone. (2S,3R)-Brassinazole might be the most active form of Brz[1][2][3].
C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM[1].
Pyrene-d10 is the deuterium labeled Pyrene[1].
Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.
Denthyrsinin is a phenanthrene[1].
AMPSO is an alkaline transfer buffer that can be used to transfer strongly basic proteins from gels into nitrocellulose without reducing the transfer efficiency of other proteins. AMPSO can be used for Western Blot analysis, PCR amplification and many other applications[1].
Citric acid is a weak organic tricarboxylic acid found in citrus fruits. Citric acid is a natural preservative and food tartness enhancer.
ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
N-Acetyl-4-hydroxy-L-proline (cis- and trans- mixture) is a proline derivative[1].
Dihydrocytochalasin B is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport[1]. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis, causes cell rounding and a loss of actin microfilament bundles[2]. Dihydrocytochalasin B is related to transcytoplasmic movement of calcium by inhibiting active calcium transport and causes a Ca+increase in the mucosal scrapings[3].
Lemzoparlimab (TJ011133; TJC4) is a humanized anti-CD47 IgG4 antibody. Lemzoparlimab has a strong anti-tumor activity[1].
N-(3-Methylbutyl)adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Competence-Stimulating Peptide-2 (CSP-2) is a quorum sensing signal peptide produced by Streptococcus pneumoniae. ComD2 is a compatible receptor of Competence-Stimulating Peptide-2 (CSP-2) with an EC50 value of 50.7 nM[1].
APD 371 is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
N-(Azido-PEG3)-N-Biotin-PEG4-methyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
Naringenin-4',7-diacetate (compound 13) is a pyrrolidinoflavanne isolated from the fruits of Vocbysiaguianensis[1].
Madolin U is a germacrane sesquiterpene isolated from the herb of Viola yedoensis[1].
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.