125256-00-0 Usage
Description
Fatostatin A, with the chemical formula 125256-00-0, is a cell-permeable inhibitor that specifically targets the activation of SREBP (Sterol Regulatory Element-Binding Protein). It functions by blocking adipogenesis, the process of cell differentiation into adipocytes, which are fat-storing cells. Fatostatin A achieves this by inhibiting the ER-Golgi translocation of SREBPs, a process that is facilitated by their escort protein, SCAP. Fatostatin A has demonstrated the ability to prevent increases in body weight, blood glucose, and hepatic fat accumulation in obese ob/ob mice. Additionally, it has been shown to inhibit high glucose-induced TGF-β in mesangial cells, making it a promising candidate for various therapeutic applications.
Uses
Used in Pharmaceutical Industry:
Fatostatin A is used as a therapeutic agent for the treatment of obesity and related metabolic disorders. Its ability to inhibit the activation of SREBP and block adipogenesis makes it a potential candidate for managing body weight, blood glucose levels, and hepatic fat accumulation in obese patients.
Used in Research Applications:
Fatostatin A is used as a research tool for studying the role of SREBP in cellular processes, particularly in adipogenesis and lipid metabolism. Its cell-permeable property allows researchers to investigate the underlying mechanisms of SREBP activation and its impact on cellular functions.
Used in Drug Development:
Fatostatin A serves as a lead compound in the development of new drugs targeting obesity and metabolic disorders. Its inhibitory effects on SREBP activation and adipogenesis make it a valuable starting point for designing novel therapeutic agents with improved efficacy and safety profiles.
Used in Cell Biology:
Fatostatin A is used as a cell biology tool to understand the role of SREBP in cellular differentiation and the development of adipose tissue. By inhibiting SREBP activation, researchers can gain insights into the molecular pathways involved in adipogenesis and identify potential targets for therapeutic intervention.
References
1) Kamisuki et al. (2009), A small molecule that blocks fat synthesis by inhibiting the activation of SREBP; Chem. Biol., 16 882
2) Uttarwar et al. (2012), SREBP-1 activation by glucose mediates TGF-β upregulation in mesangial cells; Am. J. Physiol. Renal Physiol., 302 F329
Check Digit Verification of cas no
The CAS Registry Mumber 125256-00-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,5,2,5 and 6 respectively; the second part has 2 digits, 0 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 125256-00:
(8*1)+(7*2)+(6*5)+(5*2)+(4*5)+(3*6)+(2*0)+(1*0)=100
100 % 10 = 0
So 125256-00-0 is a valid CAS Registry Number.
125256-00-0Relevant articles and documents
Diarylthiazole: An antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system
Bellale, Eknath,Naik, Maruti,Vb, Varun,Ambady, Anisha,Narayan, Ashwini,Ravishankar, Sudha,Ramachandran, Vasanthi,Kaur, Parvinder,McLaughlin, Robert,Whiteaker, James,Morayya, Sapna,Guptha, Supreeth,Sharma, Sreevalli,Raichurkar, Anandkumar,Awasthy, Disha,Achar, Vijayshree,Vachaspati, Prakash,Bandodkar, Balachandra,Panda, Manoranjan,Chatterji, Monalisa
, p. 6572 - 6582 (2014/10/15)
Diarylthiazole (DAT), a hit from diversity screening, was found to have potent antimycobacterial activity against Mycobacterium tuberculosis (Mtb). In a systematic medicinal chemistry exploration, we demonstrated chemical opportunities to optimize the potency and physicochemical properties. The effort led to more than 10 compounds with submicromolar MICs and desirable physicochemical properties. The potent antimycobacterial activity, in conjunction with low molecular weight, made the series an attractive lead (antibacterial ligand efficiency (ALE) >0.4). The series exhibited excellent bactericidal activity and was active against drug-sensitive and resistant Mtb. Mutational analysis showed that mutations in prrB impart resistance to DAT compounds but not to reference drugs tested. The sensor kinase PrrB belongs to the PrrBA two component system and is potentially the target for DAT. PrrBA is a conserved, essential regulatory mechanism in Mtb and has been shown to have a role in virulence and metabolic adaptation to stress. Hence, DATs provide an opportunity to understand a completely new target system for antimycobacterial drug discovery.
