srebp

MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist. It potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level. MSU-42011 has demonstrated antitumor activity in a [kras]-driven mouse model of lung cancer and is effective for the treatment of preclinical [kras]-driven lung cancer with immunomodulatory activity.

PF-429242 is a competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). It is selective for site 1 protease against a panel of serine proteases. PF-429242 inhibits rate of cholesterol synthesis in CHO c

Fatostatin is a specific inhibitor of SREBP activation, it impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs.

Icariside E4 is a natural compound derived from Ulmus minor that acts via AMPK phosphorylation and inhibition of MID1IP2 hypolipidation in HepG1 cells.Icariside E4 has anti-injurious, antioxidant, anti-Alzheimer's and anti-inflammatory effects and inhibits SREBP-1c, liver X receptor-α (LXR) and FASN in Icariside E4 is an effective candidate for the treatment of fatty liver disease and has hypolipidemic potential in HepG1 cells.

SREBP/SCAP-IN-2 (compound 13) acts as a selective inhibitor of SREBP/SCAP [1].

SREBP/SCAP-IN-1 (compound 10b) serves as a selective inhibitor of SREBP/SCAP [1].

Betulin (betulinol) (lup-20(29)-ene-3β, 28-diol) is an abundant, naturally occurring triterpene. It is commonly isolated from the bark of birch trees where it forms up to 30% of the dry weight of the extractive and is found in birch sap as well.

Methyl cinnamate, a tyrosinase inhibitor and a flavoring compound, has antimicrobial, antiadipogenic, vasorelaxant, and anti-inflammatory effects.

4-Hydroxyflavanone is a natural product, shows full vasorelaxing effects

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.

Fatostatin hydrobromide (Fatostatin A HBr) ia an inhibitor of sterol regulatory element binding protein (SREBP). It impairs the activation of SREBP-1 and SREBP-2.

Praeruptorin B (Praeruptorin D), a compound found in the roots of Peuced, is an inhibitor of sterol regulatory element-binding proteins (SREBPs) that attenuates the metastatic ability of human renal cancer cells by targeting CTSC and CTSV expression, and can be used in the study of osteoporosis.

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

FGH10019 is a novel inhibitor of sterol regulatory element-binding protein (SREBP) ( IC50 :1 μM).

Hexacosanol activates AMPK and hepatic autophagy and inhibits SREBP2, resulting in hypocholesterolemic activities and improvement of hepatic steatosis.

PF429242 dihydrochloride is a reversible and competitive inhibitor of S1P, with an IC50 of 175 nM.

Nicodicosapent is a fatty acid niacin conjugate and an inhibitor of the sterol regulatory element-binding protein (SREBP), which is a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.

SIRT6 activator2 (compound 31) is a sirtuin6 activator known for its anti-lipid accumulation properties. It significantly downregulates LXR, SREBP-1c, and their target genes, making it valuable for research into lipid metabolism-related diseases.

Betulinditosylate is a derivative of Betulin, which functions as an SREBP inhibitor.

HSD17B13-IN-104 (Compound 32) is an orally active and potent inhibitor of HSD17B13 with high selectivity (IC50=2.5 nM). It modulates liver lipid metabolism by inhibiting the SREBP-1c/FAS pathway and blocks the enzymatic activity of HSD17B13 to alleviate hepatic lipid accumulation. HSD17B13-IN-104 shows potential for research in metabolic dysfunction-associated fatty liver disease.

Elsulfavirine sodium (R-1206 sodium) is an orally effective inhibitor of human carbonic anhydrase (CA) and an allosteric inhibitor of HIV-1 non-nucleoside reverse transcriptase (NNRT). It targets and disrupts the interaction between adenylosuccinate lyase (ADSL) and insulin-induced gene proteins INSIG1/2, blocking SREBP-1-mediated de novo lipid synthesis and inhibiting liver cancer cell proliferation. In combination with Lenvatinib, Elsulfavirine sodium exhibits synergistic antitumor effects. Inside the body, it converts to the active metabolite VM1500A, which blocks reverse transcriptase DNA polymerization activity, thereby inhibiting HIV-1 replication. The Ki values for Elsulfavirine sodium against human carbonic anhydrase subtypes I, VII, VI, VA, VB, IX, XIII, XIV range from 1960 nM to 52400 nM. This compound is utilized in research related to HIV-1 infection and liver cancer.

O-1602 is a novel GPR55 agonist, an atypical cannabinoid associated with the central nervous system and obesity, and is a candidate compound for the treatment of cystitis.O-1602 promotes hepatic steatosis through GPR55 and PI3 kinase / Akt / SREBP-1c signalling in mice.O-1602 induces, in a GPR3-independent manner, in Hep55B cells with elevated intracellular calcium.

Phillyrin (Forsythin) is a novel AMPK activator, has anti-obesity effects in nutritive obesity mice, it can prevent lipid accumulation in HepG2 cells by blocking the expression of SREBP-1c and FAS through LKB1/AMPK activation. Phillyrin(Forsythin) may be a new preventive agent of acute lung injury in the clinical setting, it potentially contributes to the suppression of the activation of MAPK and NF-κB pathways, it also has protective effects on H2O2-induced oxidative stress and apoptosis in PC12 cells.

Dihydrocurcumin is the main metabolite of curcumin, which can reduce fat accumulation and oxidative stress response. Dihydrocurcumin can regulate the mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increase the protein expression levels of pAKT and PI3K, and reduce the intracellular NO and ROS contents through Nrf2 signaling pathway.