Nadolol D9 is the deuterium labeled Nadolol(SQ-11725), which is a non-selective beta blocker.
Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.IC50 value:Target: Difluprednate ophthalmic emulsion 0.05% is also being studied in other ocular inflammatory diseases, including a U.S. Phase 3 study evaluating difluprednate for the treatment of anterior uveitis.
N-Azido-PEG4-N-Boc-N-PEG3-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
Liriopesides B (Nolinospiroside F) is a steroidal saponin isolated from Ophiopogon japonicas. Liriopesides B has anti-oxidative and anti-aging effects[1].
Buformin (1-Butylbiguanide) is a potent and orally active biguanide antidiabetic agent, an AMPK activator. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al)[1].
(2S)-4'-Hydroxy-7-methoxyflavan is a Flavan. Flavan (4′-hydroxy-7-methoxyflavan) showed an important cytotoxic effect on human leukemic Molt 4 cells[1].
CJ-42794 is a selective prostaglandin E receptor subtype 4(EP4) antagonist, inhibits [3H]-PGE2 binding to the human EP4 receptor with a mean pKi of 8.5, a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3).IC50 value: 8.5 (pKi ) [1]Target: EP4in vitro: CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor with a mean pA2 value of 8.6. PGE2 inhibits the lipopolysaccharide (LPS)-induced production of tumor necrosis factor α (TNFα) in human whole blood (HWB); CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner. [1]in vivo: CJ-42794 significantly delays the ulcer healing in rats and mice. The expression of VEGF in primary rat gastric fibroblasts was increased by PGE2 or AE1-329 (EP4 agonist), and these responses were both attenuated by coadministration of CJ-42794.[2]
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) is an orally active inhibitor of Angiotensin converting enzyme (ACE), with an inhibiton rate of 48% at 50 μM. H-Tyr-Phe-OH can be used as an biomarker for differentiating benign thyroid nodules (BTN) from thyroid cancer (TC). H-Tyr-Phe-OH exhibits xanthine oxidase inhibition (uric acid lowering) activity and serves as regulator in IL-8 production in neutrophil-like cells[1][2][3][4].
Arg-Trp is a dipeptide composed of arginine and tryptophan, and analogues of Arg-Trp-octyl ester show antibacterial activity[1].
Mocravimod is an oral activity amphematoshenol-1-1-phosphate receptor (S1PR) regulator, which can block the required signal from lymph organs to prevent the migration of effect cells from migrating to non-lymph hematopoietic tissue. Mocravimod can be used for cancer research[1].
A novel potent, selective Mcl-1 inhibitor with IC50 of <3 nM in FRET assays; displays >1,000-fold selectivity over Bcl-2 and Bcl-xL; induces cleaved caspase-3 in MV4-11 cells with IC50 of 3.78 uM.
Pantethine is a dimeric form of pantothenic acid, is an intermediate in the production of Coenzyme A, is available as a dietary supplement, and is used to treat acne and improve the blood-cholesterol profile.
Cordycepin, which is a nucleoside derivative isolated from Cordyceps, inhibits IL-1β-induced MMP-1 and MMP-3 expression in rheumatoid arthritis synovial fibroblasts (RASFs) in a dose-dependent manner.
Propargyl-PEG7-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor for Src, eEF2-K, and PKA, and EGFR-K/PKC. TX-1123 is a cyclo-oxygenase (COX) inhibitor with IC50 values of 1.16 μM and 15.7 μM for COX2 and COX1, respectively. TX-1123 has low mitochondrial toxicity. TX-1123 can be used in research of cancer[1][2].
15-Keto latanoprost is a metabolite of Latanoprost, which is an ocular hypotensive agent[1].
Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
Capadenoson is a selective agonist of adenosine-A1 receptor.
6-(4-Methoxyphenyl)pyridazin-3-amine is an aminopyridazine derivative, and can be used for the synthesis of SR 95103. SR 95103 is a selective and competitive GABA-A receptor antagonist[1].
Lirentelimab (AK002) is a humanized IgG1 monoclonal antibody that targets sialic acid-binding Ig-like lectin 8 (SIGLEC8). Lirentelimab induces cell Apoptosis of IL-5-activated eosinophils and inhibits IgE-mediated mast cell activation. Lirentelimab can be used for the research of eosinophilic gastritis and duodenitis[1].
Aspartame acesulfame is a methyl ester of a dipeptide. Aspartame acesulfame can be used as a synthetic nonnutritive sweetener. Aspartame acesulfame is composed of phenylalanine (50%), aspartic acid (40%) and methanol (10%)[1][2].
Glycyrrhizin-6'-methylester is a natural product that can be isolated from licorice (Glycyrrhiza glabra)[1].
PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).IC50 value: 4.8 nM [1]Target: in vitro: Being more selective than staurosporine or PF-02341066, PF-04217903 displays >1000-fold selectivity for c-Met over a panel of 208 kinases, although more susceptible to oncogenic mutations of c-Met that attenuate potency than PF-02341066. In addition to WT c-Met, PF-04217903 displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM [1]. PF-04217903 in combination with sunitinib significantly inhibits endothelial cells, but not the tumor cells B16F1, Tib6, EL4, and LLC [2] PF-04217903 significantly inhibits the clonogenic growth of LXFA 526L and LXFA 1647L with IC50 values of 16 nM, and 13 nM, respectively, yielding an additive effect when in combination with cetuximab [3]. in vivo: Although unable to inhibit tumor growth in the sunitinib-sensitive B16F1 and Tib6 tumor models, the combination of PF-04217903 and sunitinib significantly inhibits tumor growth in sunitinib-resistant EL4, and LLC tumor models compared with sunitinib or PF-04217903 alone by significantly blocking vascular expansion, indicating a functional role for HGF/c-Met axis in the sunitinib-resistant tumors [2].
Hypoxanthine-13C5,15N4 is a 15N-labeled and 13C-labled Dansyl chloride.
BnO-PEG1-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
DMT-2'O-Methyl-rU Phosphoramidite (2'-O-Me-U Phosphoramidite) is a 2'-O-Me derivative, and can be used for oligonucleotide synthesis[1][2].
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8[1].
(RS)-S-Adenosyl-L-methionine-d3(S-methyl-d3) Tetra(p-toluenesulfonate) Salt is the deuterium labeled (RS)-S-Adenosyl-L-methionine Tetra(p-toluenesulfonate) Salt[1].
19-Hydroxybaccatin III is a compound isolated from the leaves and twigs of Taxus sumatrana[1].