aggressive

Azobenzene is a phototrigger that can be used to design and synthesize a variety of photoresponsive systems.Azobenzene is genotoxic and induces aggressive sarcomas of the spleen and other abdominal organs.

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM. Kd of UPGL00004 for GAC was 27 nM. UPGL00004 has a strong inhibitory effect on the proliferation of highly aggressive triple negative breast cancer cell lines.

U 99194 maleate (U-99194A maleate) is a D3 antagonist and increases social behaviors of isolation-induced aggressive male mice.

Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.

GTCpFE, a compound synthesized from Dimethyl fumarate (DMF) and Aspirin (ASA), inhibits IKKα β in the NF-κB pathway, exhibiting anti-inflammatory activity by preventing p65 from entering the nucleus. It selectively inhibits cancer stem cell (CSC) activity by reducing the growth of mammospheres and the expression of the CD44+CD24- immune phenotype. Furthermore, GTCpFE targets breast cancer stem cells, crucial in aggressive cancer phenotypes that depend on NFκB and PGE2.

Selprazine was developed as a sedative to inhibit aggressive behavior.

Fluprazine (originally known as DU27716) is a psychoactive compound that was studied for its potential as a behaviorally selective anti-aggressive agent.

Naprodoxime HCl is an antidepressant. It also is an anti-aggressive agent.

SR 57227A is a highly selective of peripheral and central 5-HT3 receptors and an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It exhibits anti-depressant like effects in rats and decreased isolation-induced aggressive beh

Nefazodone hydrochloride (Serzone) is a serotoninergic modulating antidepressant that is used in therapy of depression, aggressive behavior and panic disorder.

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A/1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg/kg i.p.) or eltoprazine (1 mg/kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor (IC50 = 20 nM) that regulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells [1].

HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor (IC50 = 58 nM) that regulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells [1].

CDK7-IN-2 is a potent inhibitor of CDK7, which plays a role in transcription initiation via phosphorylation of the Rbpl subunit of RNA polymerase II (RNAPII). CDK7 is linked to the temporal control of the cell cycle and transcriptional activity, and has research potential for aggressive and difficult-to-treat cancers.

XP-524 is a potent inhibitor of BET and EP300. XP-524 has significant tumouricidal effects in vivo, preventing KRAS-induced tumour transformation in vivo and prolonging survival in two aggressive PDAC transgenic mouse models. XP-524 also enhances the expression of its own peptide and recruitment of tumour cells to cytotoxic T lymphocytes. XP-524 has shown potential for research in pancreatic ductal adenocarcinoma (PDAC).

Anpirtoline free base is a highly potent 5-HT1B receptor agonist. Anpirtoline has been shown to decreases central serotonin synthesis and attenuate aggressive behavior in vivo. Anpirtoline also acts as an antagonist at 5-HT3 receptors and can bypass the blood-brain barrier.

STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, in an aggressive syngeneic model, demonstrated superior tumor growth inhibition and a positive therapeutic index relative to combretastatin A-4 phosphate (CA4P).

Maprotiline-d3 is intended for use as an internal standard for the quantification of maprotiline by GC- or LC-MS. Maprotiline is a tricyclic antidepressant. It binds to the norepinephrine transporter (NET) and is selective for NET over the serotonin and dopamine transporters. Maprotiline also binds to the serotonin (5-HT) receptor subtype 5-HT2A, as well as histamine H1, muscarinic acetylcholine, α1-adrenergic, and dopamine D2 receptors. In vivo, maprotiline inhibits norepinephrine reuptake in rat brain and peripheral tissues. It reduces isolation-induced aggressive behavior and inhibits electrical foot-shock stimulation-induced belligerence in mice when administered at doses ranging from 3 to 10 mg kg. Maprotiline also reduces aggressive behavior in rhesus monkeys housed in groups. Formulations containing maprotiline have been used in the treatment of depression and anxiety.

HDAC10-IN-2 hydrochloride (compound 10c) is a highly potent and selective HDAC10 inhibitor with an IC50 of 20 nM, influencing autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells [1].

4A3-SC8 is a modular dendritic macromolecule with cationic and lipophilic groups that enables small RNAs to prolong survival in an aggressive hepatocellular carcinoma model and can be used to synthesize lipid nanoparticles.

Tisagenlecleucel (CTL019), an autologous anti-CD19 chimeric antigen receptor (CAR) T-cell therapy, selectively targets and eradicates CD19-expressing B cells, and is utilized in the study of refractory aggressive diffuse large B-cell lymphoma [1] [2].

AS115, a potent and selective KIAA1363 inactivator, exhibits an IC50 of 150 nM. It targets KIAA1363, a 2-acetyl monoacylglycerol ether (MAGE) hydrolase, which is notably upregulated in aggressive cancers across diverse tissues [1] [2].