Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor[1][2].
VTP-27999 2,2,2-trifluoroacetate is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.Ic50 value:Target: Renin
Kushenol L is one of the main components of EtOA cextracts from Kushen, a traditional medicinal herb derived from the dried roots of Sophora flavescens Ait. Kushenol L is a flavonoid and plays an important role in anti-diabeticeffects[1].
N6-Methyladenosine N1-oxide is an adenosine analogue. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. The popular products in this series are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory[1][2][3].
HDAC6 degrader-3 is a potent and selective HDAC6 degrader via ternary complex formation and the ubiquitin-proteasome pathway with a DC50 value of 19.4 nM. HDAC6 degrader-3 has IC50s of 4.54 nM and 0.647 μM for HDAC6 and HDAC1, respectively. HDAC6 degrader-3 causes strong hyperacetylation of α-tubulin[1].
Fluorescein-PEG6-bis-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
A small molecule autophagy enhancer that specificly inhibits myotubularin-related phosphatase MTMR14; at concentrations of 2, 10, and 100 uM, AUTEN-67 inhibits MTMR14 by nearly 3%, 25%, and 70%, respectively; shows no activity for CDC25B , other phosphatase, PTPN1; significantly increases autophagic flux in cell lines and in vivo models, promotes longevity and protects neurons from undergoing stress-induced cell death; also restores nesting behavior in a murine model of Alzheimer disease, without apparent side effects.
MST-312 is a telomerase inhibitor. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 can be used for the research of cancer, such as multiple myeloma (MM)[1].
2'-O-Methyladenosine, a methylated adenine residue is found in urine of normals as well as in urine of adenosine deaminase (ADA) deficient patients. 2'-O-Methyladenosine exhibits unique hypotensive activities [1][2].
Fmoc-Thr(tBu)-OPfp is a threonine derivative[1].
Hydroxy-PEG3-NHS is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
MGB-BP-3 is an antibiotic that has been shown to be active against a broad range of important multi-resistant Gram-positive pathogens.
SCO-PEG3-NH2 is a cleavable ADC Linker containing 3 PEG units. SCO-PEG3-NH2 can be used as a copper-free click chemical reagent for catalyst-free click reactions.
Bruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity[1][2].
Acyclovir, a molecule tailored to inactivate the thymidine kinase of the herpesvirus, is a guanosine analogue antiviral drug. It is a drug for HSV infection by GlaxoSmithKline.IC50 Value: 0.53-0.75 uM [3]Target: HSVin vitro: Acyclovir sensitivity was determined in a plaque-reduction assay in Vero cells. IC50 Values were consistently 2-3 fold lower in B2 compared with the H strain of Vero cells. HSV Type 2 strains were 2-10-fold less sensitive than Type 1 strains [2]. in vivo: two patients experienced a recurrence during treatment with oral acyclovir (200 mg 4 times daily) for up to 12 weeks, compared with nine during placebo treatment (P = 0.016). There was no difference between acyclovir and placebo in the time to the next recurrence following completion of treatment [3]. low-dose oral acyclovirmay be effective in the prevention of HSV infection during OKT3 treatment of seropositive patients. Continuation of acyclovir prophylaxis for two to four weeks following the conclusion of OKT3 therapy may prevent occurrence of delayed infections [4].Clinical trial: Acyclovir to Treat Patients Co-infected With HIV and Herpes Viruses in Uganda. Phage2
U-54494A is a benzamide derivative related to κ-opioid receptor agonists, U-54494A has an anticonvulsant activity[1].
Emtricitabine triphosphate tetrasodium salt is the tetrasodium salt form of Emtricitabine triphosphate (HY-131596). However，Emtricitabine triphosphate ((-)-Emtricitabine triphosphate) is the phosphorylated anabolite of Emtricitabine (HY-17427)，a nucleoside reverse transcriptase inhibitor，targeting to HIV and HBV[1].
Fosravuconazole is a prodrug of ravuconazole, with antifungal activity.
N-Eicosane-d42 is the deuterium labeled N-Eicosane[1].
Carbobenzoxyproline (L-Cbz-Proline) is an inhibitor of prolidase. Carbobenzoxyproline can be used for prolidase deficiency (PD) research[1].
CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].
2-Amino-4,4,4-trifluorobutyric acid is an alanine derivative[1].
Oxyphyllenone A is an inhibitor of NO Synthase. Oxyphyllenone A inhibits the NO production in lipopolysaccharide-activated macrophages with an IC50 of 28 μM[1].
Indole-3-carboxaldehyde (3-Formylindole), a cabbage extract, is the product of the oxidative degradation of indole-3-acetic acid (IAA) by crude enzyme preparations from etiolated pea seedlings. Indole-3-carboxaldehyde (3-Formylindole) is a biochemical used to prepare analogs of the indole phytoalexin cyclobrassinin[1].
Magnesium citrate is a magnesium salt form that provides efficient penetration into brain and muscle tissue. Magnesium citrate increases pain threshold and reduces TLR4 concentration in the brain. Orally active[1].
ARN726 is a potent, selective, orally bioavailable N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 63 nM (r-NAAA) and 27 nM (h-NAAA); shows no interaction with a panel of 28 biologically relevant targets comprising lipid-metabolizing and inflammation-related enzymes; exerts profound anti-inflammatory effects in both mouse models and human macrophages.
Boscalid is an anti-fungal agent. Boscalid is a succinate dehydrogenase (SDH) inhibitor[1].
Thiabendazole inhibites the mitochondrial helminth-specific enzyme, fumarate reductase, with anthelminthic property. Target: Fumarate ReductaseTiabendazole serves to block angiogenesis in both frog embryos and human cells. It has also been shown to serve as a vascular disrupting agent to reduce newly established blood vessels. Tiabendazole has been shown to effectively do this in certain cancer cells. Thiabendazole works by inhibition of the mitochondrial, helminth-specific enzyme, fumarate reductase, with possible interaction with endogenous quinone [1].Thiabendazole inhibited B16F10 proliferation in vitro in a dose- and time-dependent manner with an IC50 of 532.4 +/- 32.6, 322.9 +/- 28.9, 238.5 +/- 19.8 microM at 24, 48, and 72 h, respectively. Moreover, thiabendazole inhibited the angiogenesis and the migration of B16F10 cells in vitro. Furthermore, thiabendazole restrained transcription and translation of the VEGF gene in B16F10 in vitro, and the apoptotic percentage of B16F10 cells was increased after exposure to thiabendazole [2].