dominant

Methyl 2-hydroxy-4-methylvalerate [Methyl 2-hydroxyisovalerate] is a predominant volatile compound found in Zhenjiang aromatic vinegar.

2-Methylcinnamic acid, predominantly trans is a useful organic compound for research related to life sciences. The catalog number is T65873 and the CAS number is 2373-76-4.

3-Bromocinnamic acid, predominantly trans is a useful organic compound for research related to life sciences and the catalog number is T67378.

3,5-Dimethoxycinnamic acid, predominantly trans is a useful organic compound for research related to life sciences. The catalog number is T67479 and the CAS number is 16909-11-8.

EMD57033 is a cardiac troponin C (cTnC) activator, a dominant Ca2+ sensitizer, which functions by binding to cardiac/slow skeletal troponin C heterodimers to promote cardiac contraction.

4-Hydroxyphenylpyruvic acid is an enzyme inhibitor.4-Hydroxyphenylpyruvic acid (4-HPPA) is a keto acid that is involved in the tyrosine catabolism pathway. It is a product of the enzyme (R)-4-hydroxyphenyllactate dehydrogenase (EC 1.1.1.222) and is formed during tyrosine metabolism. The conversion from tyrosine to 4-HPPA is catalyzed by tyrosine aminotransferase. Additionally, 4-HPPA can be converted to homogentisic acid which is one of the precursors to ochronotic pigment. The enzyme 4-hydroxyphenylpyruvic acid dioxygenase (HPD) catalyzes the reaction that converts 4-hydroxyphenylpyruvic acid to homogentisic acid. A deficiency in the catalytic activity of HPD is known to lead to tyrosinemia type III, an autosomal recessive disorder characterized by elevated levels of blood tyrosine and massive excretion of tyrosine derivatives into urine. It has been shown that hawkinsinuria, an autosomal dominant disorder characterized by the excretion of 'hawkinsin,' may also be a result of HPD deficiency . Moreover, 4-hydroxyphenylpyruvic acid is also found to be associated in phenylketonuria, which is also an inborn error of metabolism. There are two isomers of HPPA, specifically 4HPPA and 3HPPA, of which 4HPPA is the most common.

DM-4107 is a primary metabolite of Tolvaptan, primarily metabolized by the CYP3A4 enzyme in the liver. In SCHH cells, DM-4107 inhibits the human liver transport proteins NTCP, BSEP, MRP3, and MRP4, with IC50 values of 95.6, 119, 61.2, and 37.9 μM respectively, affecting bile acid transport. It is applicable for research on autosomal dominant polycystic kidney disease (ADPKD).

HDAC6-IN-43 (compound 26) is a potent inhibitor of HDACs. This compound effectively inhibits various HDACs, notably HDAC1, HDAC2, and HDAC6, with an IC50 of less than 150 nM, and demonstrates particularly high sensitivity to HDAC6 with an IC50 of 11 nM. HDAC6-IN-43 is utilized in the study of autosomal dominant polycystic kidney disease (ADPKD).

TBK1degrader-4 (Compound 30) is a molecular glue degrader targeting TBK1. It effectively inhibits cyst growth, reduces inflammation, and lowers levels of pro-inflammatory factors such as Ccl2, IFNβ, and IL-6. TBK1degrader-4 shows potential for research in autosomal dominant polycystic kidney disease (ADPKD).

DM-4103 is a primary metabolite of Tolvaptan, predominantly metabolized by the CYP3A4 enzyme in the liver. In SCHH cells, DM-4103 inhibits the human liver transport proteins NTCP, BSEP, MRP2, MRP3, and MRP4 with IC50 values of 16.3, 4.15, 51.0, 44.6, and 4.26 μM, respectively, and affects bile acid transport. DM-4103 is applicable for research in autosomal dominant polycystic kidney disease (ADPKD).

AXT-914 is an inhibitor of the calcium-sensing receptor (CaSR). It exhibits antiviral activity against coronaviruses HCoV 229E and SARS-CoV2. AXT-914 reduces cytoplasmic calcium signaling activity caused by CaSR mutations. It is applicable in research on Bartter syndrome type 5, autosomal dominant hypocalcemia (ADH), and coronavirus infections.

Brr2-IN-3 (Brr2 Inhibitor C9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa (a group of progressive retinal degenerative disorders).

Photoregulin1 is a modulator of Nr2e3. Photoregulin1 slows the progression of photoreceptor degeneration in two common mouse models of autosomal dominant RP, the RhoP23H and the Pde6brd1 mutations.

Hexyl decanoate, the first trail pheromone compound identified in a stingless bee, Trigona recursa. Hexyl decanoate is dominant component of gland secretions.

Nanangenine B is a drimane sesquiterpene that has been found inAspergillus.1It is active againstB. subtilis(IC50= 62 μg/ml) and cytotoxic to NS-1 mouse myeloma cells (IC50= 38 μg/ml). 1.Lacey, H.J., Gilchrist, C.L.M., Crombie, A., et al.Nanangenines: Drimane sesquiterpenoids as the dominant metabolite cohort of a novel Australian fungus, Aspergillus nanangensisBeilstein J. Org. Chem.152631-2643(2019)

Nanangenine F is a drimane sesquiterpene fungal metabolite that has been found inA. nanangensis.1It is active againstB. subtilis(IC50= 78 μg/ml) and cytotoxic to NS-1, DU145, and MCF-7 cancer and NFF non-cancerous cells (IC50s = 49, 95, 49, and 84 μg/ml, respectively). 1.Lacey, H.J., Gilchrist, C.L.M., Crombie, A., et al.Nanangenines: Drimane sesquiterpenoids as the dominant metabolite cohort of a novel Australian fungus, Aspergillus nanangensisBeilstein J. Org. Chem.152631-2643(2019)

Nanangenine G is a drimane sesquiterpene that has been found inAspergillus.1It is cytotoxic to NS-1 mouse myeloma cells (IC50= 47 μg/ml). 1.Lacey, H.J., Gilchrist, C.L.M., Crombie, A., et al.Nanangenines: Drimane sesquiterpenoids as the dominant metabolite cohort of a novel Australian fungus, Aspergillus nanangensisBeilstein J. Org. Chem.152631-2643(2019)

Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 |Nugent et al (2001) Potentiation of glucose uptake in 3T3-L1 adipocytes by PPARγ agonists is maintained in cells expressing a PPARγ dominant-negative mutant: evidence for selectivity in the downstream responses to PPARγ activation. Mol.Endocrinol. 15 1729 PMID:11579205 |Way et al (2001) Adipose tissue resistin expression is severely suppressed in obesity and stimulated by peroxisome proliferator-activated receptor γ agonists. J.Biol.Chem. 276 25651 PMID:11373275

Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant inhibitor of glucosylceramide synthase (GCS) utilized in the investigation of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.

GFB-12811 is an orally active, selective, and potent CDK5 inhibitor, used in the study of autosomal dominant polycystic kidney disease.

Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM, used in the treatment of autosomal dominant polycystic kidney disease (ADPKD).

Dicetrorelix pamoate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently luteinization as indicated by rising progesterone levels. Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. Cetrorelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion. It competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner......

CDK7-IN-20 is a potent, selective, and irreversible inhibitor of Cyclin-Dependent Kinase 7 (CDK7) with an IC50 value of 4 nM, exhibiting over 206-fold selectivity against related kinases [CDK1, CDK2, CDK3, CDK5, CDK6, CDK9, and CDK12]. It holds potential for research into autosomal dominant polycystic kidney disease (ADPKD).

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.