Fatty Acid Synthase
Fatty acid synthase (FASN) is a homodimeric protein; each monomer is a large polypeptide comprised of six separate enzymatic domains working in concert to synthesize the 16-carbon saturated fatty acid palmitate from building blocks of acetyl-CoA and malonyl-CoA. FASN also can localize to intracellular membranes; the specific impact of this partitioning on the cell’s function remains a field of active exploration. FASN can be phosphorylated by kinases such as mammalian target of rapamycin (mTOR) and human epidermal growth factor receptor 2 (Her2) and this regulation may be important for both activity of the enzyme and its subcellular localization. The FASN enzyme may be regulated by protein-protein interactions. FASN has been shown to co-localize with caveolin-1 on the membranes of prostate cancer cells; the presence of these antigens correlates with poor prognosis, notwithstanding that the functionality of this co-localization has not been elucidated. FASN has been shown to interact physically with the protein, designated as FAMIN, on perioxosomes, driving the flux of lipid synthesis; and the thyroid hormone responsive protein Spot14 has been shown to enhance the activity of the FASN enzyme. This enzyme and de novo lipogenesis (DNL), its cognate pathway, are critical components of tumor cell survival and proliferation for a wide range of cancers.
References
1.Buckley D, et al. Pharmacol Ther. 2017;177:23–31.
References
1.Buckley D, et al. Pharmacol Ther. 2017;177:23–31.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
Fatty Acid Synthase
-
UCM05
产品货号 : M33764
cas no: 1094451-90-7
UCM05 (G28UCM) 是一种有效的脂肪酸合酶 (FASN) 抑制剂,对 HER2+ 乳腺癌具有作用活性,且在抗 HER2 耐药细胞系中具有活性。UCM05 是一种丝状温度敏感蛋白 Z (FtsZ) 抑制剂,可抑制革兰氏阳性菌 B. subtilis 生长,MIC 值为 100 μM,但对革兰氏阴性菌 E. coli 缺乏活性。 -
VY-3-135
产品货号 : M28868
cas no: 1824637-41-3
VY-3-135 是一种转移抑制剂和乙酰辅酶A合成酶 2 (ACSS2) 调节剂。 -
ACSS2-IN-2
产品货号 : M28520
cas no: 2332820-04-7
ACSS2-IN-2 是酰基辅酶A 合成酶短链家族成员 2 (ACSS2) 的抑制剂。 ACSS2-IN-2 可以抑制 ACSS2 活性,IC50 值为 3.8 nM。 ACSS2-IN-2 可用于多种疾病的研究,例如病毒感染、代谢紊乱、神经精神疾病、炎症/自身免疫性疾病和癌症。 -
IPI-9119
产品货号 : M28096
cas no: 1346564-56-4
IPI-9119 是一种口服活性、选择性且不可逆的 FASN 抑制剂 (IC50 = 0.3 nM)。 -
Fasnall
产品货号 : M27877
cas no: 929978-58-5
Fasnall 是一种选择性 FASN 抑制剂,通过其辅因子结合位点发挥作用。 Fasnall 在 HER2(+) 乳腺癌 MMTV-Neu 模型中显示出有效的抗肿瘤活性,特别是与卡铂联合使用。