SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50 values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC50=270 nM) and phosphorylated PAK2 (IC50=720 nM)[1].
4-Methylhistamine (dihydrochloride) is the potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine (dihydrochloride) has the potential for the research of immune-related diseases such as cancer and autoimmune disorders[1].
AS1411 is a quadruplex-forming oligonucleotide aptamer that targets nucleolin. It has anti-tumor activity.
Vindorosine is an alkaloid from Catharanthus trichophyllus Roots. Vindorosine relaxes renal arteries[1][2].
Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1[1].
BRD4-BD1-IN-2 is a selective BRD4-BD1 inhibitor, with an IC50 of 2.51 µM (20-times greater than that of BD2). BRD4-BD1-IN-2 can be used in studies of cancer and cardiovascular diseases[1].
piCRAC-1 is a potent, photoinducible Ca2+ release-activated Ca2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage[1].
Tricarballylic acid, a conjugate acid of a tricarballylate, is a competitive inhibitor of the enzyme aconitate hydratase (aconitase; EC 4.2.1.3) with a Ki value of 0.52 mM[1].
Arteannuin L can be isolated from Artemisia annua[1]
3,3'-Di-O-methylellagic acid-4'-O-β-D-glucopyranoside is a ellagic acid derivative that can be isolated from Dipentodon sinicus[1].
AN3199 is a PDE4 inhibitor with IC50 of 94.5 nM.IC50 value: 94.5 nM [1]Target: PDE4The detailed information please refer to Compound 11 in the reference.
Adenosine 5'-triphosphate(ATP)-d4 (ammonium salt) is the deuterium labeled Adenosine 5'-triphosphate(ATP) ammonium salt[1].
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity[1][2].
Edralbrutinib is a potent BTK inhibitor[1].
Peptide 5g is an antimicrobial peptide. Peptide 5g inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 10, 12.5 μg/mL respectively[1].
Dihydrorhodamine 123 is a fluorescent probe (λex=488 nm, λem=525 nm).
Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans[1].
Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (Ki: 160 nM)[1][2][3].
Tyrosinase (206-214), human (AFLPWHRLF), a 9-amino acid peptide, is a tyrosinase epitope. Tyrosinase (206-214), human can be recognized by HLA-A24 restricted, tumor-infiltrating lymphocytes (TIL)[1].
15,16-Epoxy-12R-hydroxylabda-8(17),13(16),14-triene is a compound isolated from the seeds of Aframomum aulacocarpos[1].
Tebuconazole is an agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively.
BDC2.5 Mimotope 1040-63 is a biological active peptide. (The TCR transgenic model (BDC2.5) mimitope was used in type 1 diabetes (T1D) study. T1D is an autoimmune disease in which T cells mediate damage to pancreatic islet b cells. T1D is caused by autoreactive T cell destruction of insulin-producing cells. BDC2.5 mimotope was utilized to support the study on antigen presentation of antigenic peptides to islet autoantigen-specific T cells.)
Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.IC50 value:Target: tubulinin vitro: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure [1]. In all cell lines tested, HTI-286 was a potent inhibitor of proliferation and induced marked increases in apoptosis. Despite similar transcriptomic changes regarding cell death and cell cycle regulating genes after exposure to HTI-286 or docetaxel, array analysis revealed distinct molecular signatures for both compounds [2].in vivo: Intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model) [1]. HTI-286 significantly inhibited growth of PC-3 and LNCaP xenografts and retained potency in PC-3dR tumors. Simultaneous castration plus HTI-286 therapy was superior to sequential treatment in the LNCaP model [2].
Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent 12/15-Lipoxygenases (LO) inhibitor. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate has the potential for the research of type 1 diabetes mellitus[1].
Acid-PEG8-S-S-PEG8-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Fmoc-L-Lys(Pryoc)-OH (N2-Fmoc-N6-[(propargyloxy)carbonyl]-L-lysine) is a click chemistry reagent containing an azide group[1].
DAMGO TFA is a μ-opioid receptor (μ-OPR ) selective agonist with a Kd of 3.46 nM for native μ-OPR[1].
Itruvone is a intermediate of 17α-ethinylestradiol (EE2) during Fenton oxidation. Itruvone has an antidepressant effect[1][2].
Protopseudohypericin, a naturally occurring naphthodianthrone, is isolated from H. perforatum. Protopseudohypericin is considered to be the biosynthetic precursor of Pseudohypericin[1][2].