FABP Inhibitor

BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with K_is of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.

BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with K_is of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.

FABPs ligand 6 (MF6) is an FABP5 and FABP7 inhibitor with K_D values of 874 nM and 20 nM, respectively. FABPs ligand 6 can be used for multiple sclerosis research.

FABP1-IN-1 (44) is a selective FABP1 inhibitor, with an IC₅₀ of 4.46 μM. FABP1-IN-1 (44) can be used for the research of NASH.

RO6806051 is a selectivity FABP4 and FABP5 inhibitor with human FABP4 K_i values of 0.011 μM and 0.23 μM, and human FABP5 K_i values of 0.086 μM and 1.17 μM. RO6806051 can be used for the research of inflammation-related diseases.

FABP4/5-IN-7 is a dual FABP4/FABP5 inhibitor, with an IC₅₀ of 0.8 μM and a K_d of 0.01 μM for FABP4, and an IC₅₀ of 1.4 μM for FABP5. FABP4/5-IN-7 inhibits lipolysis in adipocytes. FABP4/5-IN-7 inhibits MCP-1 release in macrophages. FABP4/5-IN-7 improves dyslipidemia in diet-induced obese mice. FABP4/5-IN-7 can be used in studies related to dyslipidemia.

Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.

FABP4/5-IN-5 (compound D9) is a potent inhibitor of FABP4 and FABP5,? with the IC₅₀s of 4.68 μM and 10.72 μM, respectively.FABP4/5-IN-5 plays an important role in metabolism disorder like diabetes mellitus.

FABP4-IN-3 (compound C3) is a highly selective FABP4 inhibitor (FABP4 K_i = 25 ± 3^a nM, FABP3 K_i = 15.03 μM) which exhibits a 601-fold selectivity over FABP3. FABP4-IN-3 also shows metabolic stability and potent cellular anti-inflammatory activity, making it promising to get involved in the research of metabolic disease, cardiac dysfunction and inflammation-related disease.

FABP-IN-2 is a novel FABP3 ligand. FABP-IN-2 inhibits FABP3/FABP4 with an IC₅₀ of 1.16 μM and 4.27 μM respectively.

ISX-1 is an isoxazole. ISX-1 has anti-adipogenic and pro-osteogenic activities. ISX-1 can be used for the research of osteopenia and osteoporosis.

Eriocalyxin B is a diterpenoid compound that can be isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B exhibits multiple activities, such as anti-cancer, anti-inflammatory, and inhibition of adipogenesis. Eriocalyxin B is capable of inducing apoptosis and autophagy in tumor cells. Eriocalyxin B can be used in the research of cancers, autoimmune diseases, and other conditions.

FABP4-IN-2 (Compd 10g) is a selective and orally active FABP4 inhibitor with the K_i values of 0.51 μM for FABP4, 33.01 μM for FABP3. FABP4-IN-2 can be used in the research of inflammation-related diseases.

BMS-480404 is an inhibitor of keratinocyte fatty acid-binding protein (kFABP) and adipocyte lipid-binding protein (aP2). BMS-480404 has a K_i value of 33 nM for kFABP. BMS-480404 can be used in the research of metabolic disorders.

FABP4/5-IN-6 is an orally active, potent FABP4/5 inhibitor (Ki = 0.41/2.53 μM), showing low selectivity over FABP3 (Ki = 59.72 μM). FABP4/5-IN-6 inhibits the secretion of MCP-1 and IL-6 in Lipopolysaccharides (HY-D1056) (LPS)-induced THP-1 macrophage. FABP4/5-IN-6 exhibits significant anti-inflammatory effects and attenuates LPS-induced liver injury. FABP4/5-IN-6 has low hERG inhibition (LD₅₀ > 2000 mg/kg). FABP4/5-IN-6 can be used for the study of Inflammation-related diseases.

FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC₅₀ of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models.

BMS-309403 (Standard) is the analytical standard of BMS-309403. This product is intended for research and analytical applications. BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.

FABP4/5-IN-4 (compound E1) is a potent inhibitor of FABP4 and FABP5, with the IC₅₀s of 3.78 μM and 5.72 μM, respectively. FABP4/5-IN-4 plays an important role in metabolism disorder like diabetes mellitus.

a-FABP-IN-1 (Compound 5g) is a potent and selective human adipocyte fatty acid-binding protein (a-FABP) inhibitor with a K_i below 1.0 nM. a-FABP-IN-1 inhibits the pro-inflammatory cytokine production.

FABP4-IN-6 is a FABP4 inhibitor with an IC₅₀ of 16.8 μM. FABP4-IN-6 can be used in the research of diabetes and atherosclerosis.