Hoechst stains are part of a family of blue fluorescent dyes used to stain DNA.IC50 Value:Target: These Bis-benzimides were originally developed by Hoechst AG, which numbered all their compounds so that the dye Hoechst 33342 is the 33342nd compound made by the company. There are three related Hoechst stains: Hoechst 33258, Hoechst 33342, and Hoechst 34580. The dyes Hoechst 33258 and Hoechst 33342 are the ones most commonly used and they have similarexcitation/emission spectra. Both dyes are excited by ultraviolet light at around 350 nm, and both emit blue/cyan fluorescent light around anemission maximum at 461 nm. Unbound dye has its maximum fluorescence emission in the 510-540 nm range. Hoechst dyes are soluble in water and in organic solvents such as dimethyl formamide or dimethyl sulfoxide. Concentrations can be achieved of up to 10 mg/mL. Aqueous solutions are stable at 2-6 °C for at least six months when protected from light. For long-term storage the solutions are instead frozen at ≤-20 °C.The dyes bind to the minor groove of double-stranded DNA with a preference for sequences rich in adenine andthymine. Although the dyes can bind to all nucleic acids, AT-rich double-stranded DNA strands enhance fluorescence considerably.Hoechst dyes are cell-permeable and can bind to DNA in live or fixed cells. Therefore, these stains are often called supravital, which means that cells survive a treatment with these compounds. Cells that express specific ATP-binding cassette transporter proteins can also actively transport these stains out of their cytoplasm.
3'-Hydroxyxanthyletin is a coumarin compound with antimycobacterial activities[1][2].
Trimethobenzamide hydrochloride is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
YM 254890 is a selective Gq signaling inhibitor that strongly inhibits intracellular calcium ion mobilization and serum response element (SRE)-mediated transcription stimulated by several receptors coupled to Gq, but not those coupled to Gi, Gs, or G15; also exhibits antithrombotic and thrombolytic effects in an electrically induced carotid artery thrombosis model in rats; inhibits ADP-induced platelet aggregation in human platelet-rich plasma with an IC50 of <0.6 uM by blocking the P2Y1 receptor-signal transduction pathway. Thrombosis Discontinued
Carpaine is an alkaloid isolated from Carica papaya Linn with anti-thrombocytopenic activity, exhibits potent activity in sustaining platelet counts with no acute toxicity[1].Carpaine has anti-plasmodial activity to prevent malaria[2].Carpaine affects the myocardium directly, it reduces cardiac output, stroke volume, stroke work, and cardiac power in rat, which has been studied for its cardiovascular effects[3].
VUF 8430 (dihydrobromide) is a potent and selective histamine H4 receptor agonist with a Ki of 31.6 nM and an EC50 of 50 nM[1].
Cholesterol 24-hydroxylase-IN-2 is an inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1), with the IC50 of 5.4 nM. Cholesterol 24-hydroxylase-IN-2 can be used in imaging of cholesterol 24-hydroxylase in mammals[1].
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].
Antimycobacterial agent-3 (Compound 1h) is an antimycobacterial agent against both drug-sensitive MTB strain H37Rv and drug-resistant clinical isolates (MIC: < 0.029–0.110 μM). Antimycobacterial agent-3 shows low cell cytotoxicity[1].
Propargyl-PEG9-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
Hypertrehalosemic neuropeptide (Nauphoeta cinerea) is a neuropeptide in the adipokinetic hormone/red pigment-concentrating hormone (AKH/RPCH) family, and can stimulate the synthesis of trehalose[1].
Thrombin inhibitor 7 is a potent FXIIa inhibitor with IC50 values of 28 nM, >132 µM for FXIIa and FXIa, respectively. Thrombin inhibitor 7 shows low cytotoxicity[1].
U66858 is a potent inhibitor of LTB4 production in human whole blood. U66858 also exhibits significant inhibition of lipoxygenase and TXB2 release.
Valylleucine is a biologically active peptide.
HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
L-Alanine isopropyl ester is an alanine derivative[1].
EZH2-IN-15 (SHR2554) is a EZH2 inhibitor. EZH2-IN-15 has anti-tumor activity, and can be used for research of H3K27me3-dependent tumors[1].
7-Isocarapanaubine is an indole that can be isolated from Rauwolfi vomitoria[1].
1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity[1][2].1-Naphthohydroxamic acid can induce tubulin acetylation[3].
N-Methyl-N-(t-Boc)-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ro 15-2041 is a selective platelet phosphodiesterase inhibitor with antithrombotic properties.
5-Dehydroepisterol is an episterol derivative and an intermediate in steroid biosynthesis. 5-Dehydroepisterol can be formed by C-5 sterol desaturase and converted into 24-methylenecholesterol by 7-dehydrocholesterol reductase. 5-Dehydroepisterol has anti-fungal activities[1][2].
PD-168077 maleate is a selective dopamine D4 receptor agonist, with a Ki of 9 nM.
Cefotaxime sodium salt is a third-generation cephalosporin antibiotic; broad-spectrum antibiotic with activity against numerous Gram-positive and Gram-negative bacteria.
3-(Bromomethyl)benzonitrile-d6 is the deuterium labeled 3-(Bromomethyl)benzonitrile[1].
Protoneogracillin, a furostanol glycoside, shows anti-fungal activity against the plant pathogenic fungus P.oryzae (MMDC=94.0 μM) and cytotoxic activity on K562 cancer cells (IC50=6.6 μM)[1][2].
RSV-IN-6 (Compound 53) is an anti-RSV agent targeting M2-1 protein with EC50 values of 4.4 μM and 1.3 μM against RSV-A and RSV-B strain, respectively[1].
CP-66948 is a histamine H2-receptor antagonist with gastric antisecretory activity and mucosal protective properties.
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy[1].
Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.IC50 Value: 50 nM (EC50) [1]Target: TNF-alphaNecrostatin 2 is a potent in vitro necroptosis inhibitors (exemplified by 1, EC50-0.05 uM) that also were efficacious in an animal model of ischemic stroke. Many Necroptosis inhibitor derivatives are designed for researchers.Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-a. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins).