Fuziline is a alkaloid isolated from the lateral roots of Aconitum carmichaelii[1].
TTP488 is an antagonist at the Receptor for Advanced Glycation End products, is evaluated as a potential treatment for patients with mild-to-moderate Alzheimer's disease (AD).Target: RAGEin vitro: TTP488 is an orally active, centrally acting antagonist of RAGE-RAGE ligand interaction. Chronic oral dosing of TTP488 in AD transgenic mice led to a reduction of amyloid load in the brain, improves performance on behavioral testing and normalization of electrophysiological recordings from hippocampal slices.[1]in vivo: The small molecule RAGE antagonist, TTP488, is developed by Trans-Tech Pharma. The TTP488 or control peptide is administered i.p. daily at a dose of 100 mcg/d.[3] Successful use of the RAGE inhibitor TTP488 in Phase II testing has led to a Phase III clinical trial for AD patients.[2]
1-Bromonaphthalene-d7 is the deuterium labeled 1-Bromonaphthalene[1].
κ-Carrageenan is a natural polymer which predominantly available in red seaweeds. κ-Carrageenan is an effective drug carrier to deliver curcumin in cancer cells and to induce apoptosis. κ-carrageenan serves as a potential inflammatory agent that magnifies existing intestinal inflammation[1][2].
Allosecurinine (Phyllochrysine) is a Securinega alkaloid isolated from M.indica and M.discoidea[1].
Fmoc-D-Lys(pentynoyl)-OH is a click chemistry reagent containing an azide group. Used to introduce alkyne functionality into peptides that can be further modified using Click-chemistry[1][2].
[Lys3]-Bombesin is a biological active peptide. (PET (Positron Emission Tomography) imaging of [Lys3]-bombesin is able to detect gastrin-releasing peptide receptor (GRPR) positive prostate cancer. An immunoconjugate of [Lys3]-bombesin and corresponding monoclonal antibody can specifically induce (CD64)-dependent monocyte and neutrophil-mediated lysis of small cell carcinoma.)
Desoxycorticosterone pivalate (DOCP) is a mineralocorticoid hormone and an analog of Desoxycorticosterone. Desoxycorticosterone pivalate is used for the management of canine hypoadrenocorticism[1][2].
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects[1][2].
Echinoside B is a antifungal oligoglycosides isolated from Sea Cucumber Actinopyga echinites[1].
Oxiconazole nitrate is a broad spectrum antifungal which can inhibit the growth of T. tonsurans and T. rubrum with MIC90s of 0.25 and 0.5 μg/mL, respectively.
Statine is an unusual amino acid that occurs twice in the sequence of pepstatin, a protease inhibitor that is active against pepsin and other acid proteases.
H-Cys(Bzl)-OMe.HCl is a cysteine derivative[1].
PBRM1-BD2-IN-3 (compound 12) is a potent PBRM1-BD2 inhibitor with an IC50 value of 1.1 μM. PBRM1-BD2 Inhibitor can be used to research anticancer[1].
PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction[1].
Hydroxy-PEG3-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(S)-SW IV-52 hydrochloride is a small molecule that can induce apoptosis in ovarian cancer. (S)-SW IV-52 hydrochloride has minimal single-agent activity at concentrations up to 200 μM[1].
Tr-PEG4-OH is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
Br-5MP-Fluorescein is a dye reagent for labeling of peptides and proteins[1].
STF-083010 is an Ire1 inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity.
D-myo-Inositol, 1-[(2R)-2-hydroxy-3-[(1-oxononadecyl)oxy]propyl-1,1,2,3,3-d5 hydrogen phosphate], ammonium salt (1:1) is deuterium labeled D-myo-Inositol, 1-[(2R)-2-hydroxy-3-[(1-oxononadecyl)oxy]propyl-1,1,2,3,3 hydrogen phosphate], ammonium salt (1:1).
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively[1][2].
NGD-4715 is a selective and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist .
JAK-IN-24 is a JAK inhibitor, with IC50s of 0.534 and 24 nM at the presence of 4 μM or 1mM ATP, respectively. JAK-IN-24 also inhibits PBMC IL-15 induced STAT5 phosphorylation with an IC50 of 86.171 nM[1].
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions[1][2].
NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
Terazosin Hydrochloride dihydrate is a selective alpha1-antagonist used for treatment of symptoms of benign prostatic hyperplasia (BPH).Target: Alpha-1 Adrenergic ReceptorTerazosin Hydrochloride dihydrate is an a1-selective blocker. Its inhibitory effect on prostate tumor growth may be the result of antiangiogenic activity. Terazosin Hydrochloride dihydrate is an inhibitor of α1A-AR, α1B-AR, α1D-AR and α2B-AR [1].
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor.
Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.