neurodegenerative disorder

Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor [1].

(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor.

Gedunin is an important limonoid present in several genera of the Meliaceae family, mainly in seeds. Gedunin is an Hsp90 inhibitor, and inhibits ovarian cancer cell proliferation.

AA147 (ATF6-activator-147) is a small molecule endoplasmic reticulum (ER) proteostasis regulator. The selectively activates ATF6 arm of the unfolded protein response (UPR) .It acts as a prodrug that preferentially triggers ATF6 signaling through a mechanism involving localized metabolic activation and selective covalent modification of ER resident proteins that regulate ATF6 activity.

KTD-092, a DYRK1A inhibitor, exhibits an IC50 of 22 nM against human DYRK1A. It is applicable in research related to Down syndrome (DS), Alzheimer's disease (AD), autism spectrum disorder (ASD), diabetes, and other neurodegenerative diseases.

KMS88009 is an amyloid-β aggregation inhibitor that acts by ameliorating neurodegenerative disorder.

C16 Lactosylceramide is an endogenous bioactive sphingolipid. It forms membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs), suggesting a role in cell signaling. Plasma levels of C16 lactosylceramide are elevated in insulin-resistant cattle. C16 Lactosylceramide is also upregulated in a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder.

C20 Sphingomyelin is a naturally occurring sphingolipid. Levels of C20 sphingomyelin are upregulated in the hippocampus of rats with diabetes induced by streptozotocin and in human plasma, where it is positively correlated with insulin resistance in obese humans. C20 sphingomyelin is also upregulated in the liver of a mouse model of Niemann-Pick type C1 disease [a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder]. The plasma concentration of C20 sphingomyelin is decreased in men with prostate cancer.

Mu-6S-Palm-β-Glc is a fluorogenic substrate of palmitoyl-protein thioesterase (PPT, also known as CLN1), a lysosomal hydrolase that removes long-chain fatty acyl groups from modified cysteine residues in proteins. Upon cleavage by PPT/CLN1, it releases the fluorescent moiety 4-methylumbelliferyl (4-MU). 4-MU fluorescence is pH-dependent, with excitation maxima of 320 and 360 nm at low (1.97-6.72) and high (7.12-10.3) pH, respectively, and an emission maximum ranging from 445 to 455 nM, increasing as pH decreases. This substrate is used in assays measuring PPT activity, commonly deficient in the neurodegenerative disorder known as infantile neuronal ceroid lipofuscinosis.

BRD3731 is a selective inhibitor of GSK3β, demonstrating an IC50 value of 15 nM for GSK3β and 215 nM for GSK3α. Due to its inhibitory properties, BRD3731 holds promise for investigating various medical conditions, including post-traumatic stress disorder (PTSD), psychiatric disorders, diabetes, and neurodegenerative disorders [1].

mHTT-IN-1 (Example 1) is a potent inhibitor of the mutant huntingtin protein (mHTT), which is primarily responsible for Huntington's disease (HD), an inherited autosomal dominant neurodegenerative disorder. This compound effectively reduces mHTT levels with an EC50 of 46 nM.

β-Amyloid (1-40) TFA is a major protein fragment found in the brain plaques of Alzheimer's disease patients and is commonly used to establish Alzheimer's disease models.

Casein kinase 1δ-IN-5 is a potent and selective inhibitor of protein kinase CK1δ with an IC50 value of 47 nM, and it exhibits neuroprotective and anti-inflammatory properties in vitro, supporting its application as a mechanistic probe in neurodegenerative disease research, kinase signaling studies, and inflammation-related neurological disorder investigations.

3β,5α,6β-Trihydroxycholanic acid, a metabolite derived from 5α,6β-dihydroxycholestanol, exhibits elevated levels in dried blood spots of patients diagnosed with Niemann-Pick disease type C, a neurodegenerative disorder characterized by the accumulation of cholesterol and sphingolipids in lysosomes.

Frataxin-IN-1 is an inhibitor of the mitochondrial protein Frataxin, with an inhibitory concentration (IC 50) value of 45 μM. Compound (+)-11 is utilized in research focused on Friedreich's ataxia (FRDA), a neurodegenerative disorder associated with impaired mitochondrial function and iron-sulfur cluster biogenesis.

β-Amyloid (11-22) is a peptide fragment of β-Amyloid. β-Amyloid peptide (Abeta), the primary component of amyloid plaques in the brains of Alzheimer's patients, is believed to be the cause of Alzheimer's Disease (AD), the most common neurodegenerative disease, affecting approximately 10% of the population over 60.