BTM-3566 is an OMA1 activator. BTM-3566 activates the mitochondrial stress response. BTM-3566 induces apoptosis in diffuse large B-cell lymphomas (DLBCL) cell lines[1][2].
3,3′-Diheptylthiacarbocyanine iodide is a cyanine dye for measuring membrane potential. (λex=562 nm, λem=575 nm)[1].
Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM.
Actoxumab (Anti-C. difficile Toxin A Recombinant Antibody) is a antitoxin antibody against C. difficile toxin A by neutralizing TcdA. Actoxumab prevents both the damage to the gut wall and the inflammatory response, which are associated with C. difficile. Actoxumab has synergy effect with Bezlotoxumab (HY-P9929) targeting TcdB[1].
Azido-PEG12-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Halcinonide (SQ-18566) is a high potency corticosteroid used topically in the treatment of certain skin conditions.
Butyric acid-13C1 is the 13C labeled Butyric acid. Butyric acid is a histone deacetylase (HDAC) inhibitor, with anti-tumor effects in several cancers.
(S)-2-Amino-2,3-dimethylbutanoic acid is a valine derivative[1].
(S)-BAY-293 (BAY293 S-enantiomer) is the S-enantiomer of BAY-293 as a negative control compound.
Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.IC50 Value: 0.1-3.7 nM (breast cancer cell lines) [1]Target: Apoptosis inducer; Anticancerin vitro: Trabectedin induced cytotoxicity and apoptosis in both breast cancer cells in a time and concentration-dependent manner. The expression levels of the death receptor pathway molecules, TRAIL-R1/DR4, TRAIL-R2/DR5, FAS/TNFRSF6, TNF RI/TNFRSF1A, and FADD were significantly increased by 2.6-, 3.1-, 1.7-, 11.2- and 4.0-fold by trabectedin treatment in MCF-7 cells. However, in MDA-MB-453 cells, the mitochondrial pathway related pro-apoptotic proteins Bax, Bad, Cytochrome c, Smac/DIABLO, and Cleaved Caspase-3 expressions were induced by 4.2-, 3.6-, 4.8-, 4.5-, and 4.4-fold, and the expression levels of anti-apoptotic proteins Bcl-2 and Bcl-XL were reduced by 4.8- and 5.2-fold in MDA-MB-453 cells [2]. In vitro treatment with noncytotoxic concentrations of trabectedin selectively inhibited the production of CCL2, CXCL8, IL-6, VEGF, and PTX3 by MLS primary tumor cultures and/or cell lines [3].in vivo: A xenograft mouse model of human MLS showed marked reduction of CCL2, CXCL8, CD68+ infiltrating macrophages, CD31+ tumor vessels, and partial decrease of PTX3 after trabectedin treatment [3]. The MTD of trabectedin was 700 microg/m(2) due to dose-limiting neutropaenia and the RDs in the previously treated/untreated patients were 500 and 600 microg/m(2), respectively. Most common toxicities were nausea/vomiting (67%), asthenia/fatigue (55%) and reversible ASAT/ALAT elevation (51%) [4]. Toxicity: Most common toxicities were nausea/vomiting (67%), asthenia/fatigue (55%) and reversible ASAT/ALAT elevation (51%) [4].Clinical trial: A Study to Assess the Potential Effects of Rifampin on the Pharmacokinetics of Trabectedin in Patients With Advanced Malignancies. Phase 1/2
3,6-Dihydroxyxanthone (compound 3) is a xanthone derivatives. 3,6-Dihydroxyxanthone (compound 3) has anticancer activity. 3,6-Dihydroxyxanthone (compound 3) can be used for cancer research[1].
FFA1 agonist-1 (Compound 17a) is an orally active fatty acid receptor 1 (FFA1) agonist with an EC50 of 0.75 μM. FFA1 agonist-1 can be used for type 2 diabetes mellitus research[1].
N-Nitrosopiperidine-d10 is the deuterium labeled N-Nitrosopiperidine[1].
Azido-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as the conjugate CPT-APO (CPT: Camptothecin (HY-16560)).
2-Methyltetrahydrofuran-3-one is one of the volatile constituents of roasted coffee[1].
BRL-44408 maleate is an α2A-adrenoceptor antagonist (Ki: 8.5 nM). BRL-44408 maleate has antidepressant and analgesic activity. BRL-44408 also improves cecal ligation puncture (CLP)-induced acute lung injury[1][2].
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way[1].
Mabuterol-D9 is a deuterium labeled Mabuterol. Mabuterol is an agonist of the β2-adrenergic receptor[1].
δ-Dendrotoxin is a K+ channel blocker that can be obtained from the venom of the black mamba snake. δ-Dendrotoxin can be used in the study of neurological diseases[1].
N-Ethylglycine is a Glycine (HY-Y0966) derivative[1].
Alkyne-PEG4-maleimide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA)[1].
Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against a number of enveloped and non-enveloped viruses. Umifenovir is used as an anti-influenza virus agent. Umifenovir could effectively inhibit the fusion of virus with host cells[1][2]. Umifenovir is an efficient inhibitor of SARS-CoV-2 in vitro[2]. Umifenovir shows anti-inflammatory activity[3].
(3R,5S)-Fluvastatin is the 3R,5S-isomer Fluvastatin. Fluvastatin (XU 62-320 free acid) is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1][2][3].
(R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib, Simurosertib (TAK-931) is a selective cycle 7 (CDC7) kinase inhibitor, with an IC50<0.3 nM[1].
PS-1145 is an IκB kinase (IKK) inhibitor with an IC50 of 88 nM.
Leukotriene B4 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.
4’-α-C-Methylcytidine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Allopurinol sodium is a potent xanthine oxidase inhibitor (IC50 values of 0.2 to 50 μM). Allopurinol sodium can be used for the research of hyperuricemia and gout. Antileishmanial effect[1][2].