Huntington's disease

MIND4-19 is an inhibitor of SIRT2 with antitumor activity.

Selisistat (EX-527) is a potent and specific inhibitor of the deacetylase SIRT1 (IC50 = 38 nM) and can be utilized in the study of neurological disorders such as Huntington's chorea.

BN-82451 2HCl is a dual inhibitor of COX-1 and COX-2 and can be used to study Huntington's chorea and Parkinson's disease.

HTT-D3 is an orally active, highly efficient Huntington splicing modulator. It induces HTT mRNA degradation, reduces HTT protein levels, and inhibits P-glycoprotein (P-gp) efflux. This compound can be used in Huntington's disease research.

Dalzanemdor (SAGE-718) is an NMDA receptor-positive modulator of metabolism that can be used to study Huntington's chorea, Alzheimer's disease, and cognitive dysfunction.

Rosolutamide (ALZ-003) is a curcumin analog, an orally active Nrf1 and Nrf2 activator.Rosolutamide modulates oxidative homeostasis, improves mitochondrial function and promotes autophagy, reduces mutant protein aggregation, and decreases intracellular mitochondrial reactive oxygen species (ROS) levels.Rosolutamide has been used in the study of neurodegeneration such as spinal cerebellar ataxia and Huntington disease. neurodegenerative diseases such as Huntington's disease. Regulates oxidative homeostasis.

Tetrabenazine (Ro 1-9569) is a former antipsychotic drug used to treat various movement disorders. It inhibits neurotransmitter uptake into adrenergic storage vesicles and serves as a high-affinity label for the vesicle transport system.

Dantrolene is a postsynaptic muscle relaxant by inhibiting Ca2+ ions release from sarcoplasmic reticulum stores by antagonizing ryanodine receptors.

CHDI 00484077 is a highly selective, central nervous system (CNS) permeable Class IIa HDAC inhibitor with inhibitory effects on HDAC4, HDAC5, HDAC7, and HDAC9, which improves neuronal function, and can be used to study Huntington's disease.

B2 (Linazolamide intermediate B impurity 2) promotes inclusion formation in cellular models of Huntington's disease and Parkinson's disease

1-phenyl-3,4-dihydroisochinoline (3,4-Dihydro-1-phenylisoquinoline) is a structural analog of the neurotransmitter dopamine that interacts with dopamine receptors in the central nervous system. It has been studied as a potential therapeutic agent for the treatment of neurological disorders such as Parkinson's disease, Alzheimer's disease and Huntington's chorea.

Tetrabenazine Metabolite ((-)-β-HTBZ), a vesicles monoamine transporter 2 (VMAT2) inhibitor, is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite has a high affinity for VMAT2 with a Ki of 13.4 nM. Tetrabenazine Metabolite is often used to study chorea associated with Huntington's disease and other hyperactivity disorders.

IIQLPEIVVV TFA serves as a specific inhibitor targeting the Drp1-Mff interaction. This compound discriminates between physiological and pathological fission, hindering physiological fission which leads to mitochondrial dysfunction. IIQLPEIVVV TFA is also utilized in research related to Huntington's disease.

Pyrazolo[1,5-a]pyrimidine 4h is a morpholine derivative that is a selective antagonist of the adenosine A2A receptor. It has been shown to be neuroprotective in animal models of Parkinson's disease and Huntington's chorea.

SC 51089 is a selective prostaglandin receptor PGE2 antagonist with selectivity for prostaglandin receptor subtypes and antinociceptive activity that improves motor deficits and rescues memory decline in the Huntington's disease R6 1 mouse model .

AUTEN-67 is a specific inhibitor of MTMR14 and autophagy enhancer with potent antiaging and neuroprotective effects. AUTEN-67 also delays the onset and decreases the severity of Huntington's disease.

PF-02545920, a PDE10 inhibitor, is used potentially for the treatment of Huntington's Disease.

PBT-1033 hydrochloride is a potential neuroprotective agent for the treatment of Alzheimer's disease and Huntington's disease.

SMER10 is an enhancer of the clearance of mutant aggregate-prone proteins by autophagy in mammalian cell models of Huntington's and Parkinson's disease, independent of rapamycin.

CAY10786 (GPR52 antagonist-1) is an antagonist of G protein-coupled receptor 52 (GPR52, IC50 = 0.63 μM).

A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6 2 transgenic mouse model of Huntington's disease when administered at a dose of 0.1 mg kg.[1] [2] A-971432 (0.1 mg kg per day, i.p.) decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6 2 mice. It also increases spontaneous alternation in the t-maze in aged mice when administered at a dose of 0.1 mg kg.[1] References [1].Hobson, A.D., Harris, C.M., van der Kam, E.L., et al. Discovery of A-971432, an orally bioavailable selective sphingosine-1-phosphate receptor 5 (S1P5) agonist for the potential treatment of neurodegenerative disorders. J. Med. Chem. 58(23), 9154-9170 (2015).[2]. Di Pardo, A., Castaldo, S., Amico, E., et al. Stimulation of S1PR5 with A-971432, a selective agonist, preserves blood-brain barrier integrity and exerts therapeutic effect in an animal model of Huntington's disease. Hum. Mol. Genet. 27(14), 2490-2501 (2018).

Chloroguanabenz is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz . It inhibits prion formation in yeast and mammalian cell-based assays. Chloroguanabenz reduces the levels of both soluble and aggregated forms of the truncated Huntingtin derivative Htt48 in an HEK293T cellular model of Huntington's disease.

C2-8 is an inhibitor of polyglutamine (polyQ) aggregation with IC50s of 25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively. It also limits polyQ aggregation in organotypic hippocampal slice cultures from R6 2 transgenic mice and reduces neurodegeneration dose-dependently in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg kg) decreases huntingtin aggregate size, reduces neuronal atrophy, and enhances motor performance in a rotarod test in the R6 2 transgenic mouse model of Huntington's disease.

NCT-504, a selective allosteric inhibitor of PIP4Kγ, exhibits an IC50 value of 15.8 μM. It holds promise for the investigation of Huntington's disease.