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MedKoo Cat#: 330314 | Name: Fatostatin A
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Fatostatin A is a Cell permeable inhibitor of SREBP activation. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma.

Chemical Structure

Fatostatin A
Fatostatin A
CAS#125256-00-0 (free base)

Theoretical Analysis

MedKoo Cat#: 330314

Name: Fatostatin A

CAS#: 125256-00-0 (free base)

Chemical Formula: C18H18N2S

Exact Mass: 294.1191

Molecular Weight: 294.42

Elemental Analysis: C, 73.43; H, 6.16; N, 9.52; S, 10.89

Price and Availability

Size Price Availability Quantity
25mg USD 150.00 Ready to ship
50mg USD 250.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 850.00 Ready to ship
500mg USD 1,750.00 Ready to ship
1g USD 2,850.00 Ready to ship
2g USD 4,850.00 Ready to ship
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Related CAS #
298197-04-3 (HBr) 125256-00-0 (free base)
Synonym
Fatostatin A; Fatostatin-A; FatostatinA
IUPAC/Chemical Name
2-(2-propylpyridin-4-yl)-4-(p-tolyl)thiazole
InChi Key
ZROSUBKIGBSZCG-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H18N2S/c1-3-4-16-11-15(9-10-19-16)18-20-17(12-21-18)14-7-5-13(2)6-8-14/h5-12H,3-4H2,1-2H3
SMILES Code
CC1=CC=C(C2=CSC(C3=CC(CCC)=NC=C3)=N2)C=C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2.
In vitro activity:
Together, findings suggest that FS (fatostatin) acts to inhibit growth and induce apoptosis in ER (estrogen receptor)+ breast cancer cells and tumors. The mechanism of FS action in lipid-sufficient conditions involves activation of EnRS (endoplasmic reticulum stress) and the accumulation of lipid species (Fig. 7). The source of lipids for this lipid accumulation is unclear but de novo lipogenesis genes, such as FASN (fatty acid synthase) and ACC (acetyl-CoA carboxylase), are not regulated (either up or down) by FS in lipid-containing FBS suggesting other lipogenesis regulators, such as ChREBP or LXRα, are not involved. SCAP/SREBP inhibition does not appear to be involved in FS action in these conditions as SREBP target genes were not regulated and lipid levels were not reduced. However, SCAP/SREBP inhibition has been linked to induction of EnRS18, making this pathway a potential contributor to the findings observed. Both pro-apoptotic and anti-apoptotic lipid species accumulated in response to FS. On one hand, ceramide synthesis was elevated, which contributed to the apoptotic effects of FS, while on the other, FS activated DGATs (diacylglycerol acyltransferases) and promoted accumulation of PUFA-TAGs (poly unsaturated fatty acids-triacylglycerides), which appeared to play a protective role and limit apoptosis. Overall, global changes in the lipidome in response to FS tended to favor cell death but this could be further enhanced by blocking PUFA-TAG production. Reference: Oncogenesis. 2018 Aug; 7(8): 66. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6107643/
In vivo activity:
To further corroborate the crucial role of SREBP-dependent lipogenesis in PML-loss-driven CaP growth and metastasis, this study carried out in vivo preclinical studies of fatostatin targeting SREBP in Ptenpc−/−; Pmlpc−/− mice. Fatostatin is a recently discovered SREBP chemical inhibitor that directly binds SREBP cleavage-activating protein and blocks the endoplasmic reticulum–Golgi transport and the subsequent activation of SREBP. Treatment with fatostatin for two months in Ptenpc−/−; Pmlpc−/− mice inhibited both prostate tumor growth (Fig. 6c, d) and distant lymph node metastasis (Fig. 6e and Supplementary Fig. 5c). This potent antitumor and antimetastatic activity of fatostatin is presumably due to the suppression of SREBP pathway, because fatostatin-treated Ptenpc−/−; Pmlpc−/− tumors displayed markedly lower expression of SREBP-regulated enzymes for synthesis of FA and cholesterol (Fig. 6f, g). In agreement with the crucial role of lipid metabolism in various aspects of cancer development, fatostatin-treated Ptenpc−/−; Pmlpc−/− tumors, compared with vehicle-treated tumors, displayed a drastic decrease in the frequency of mitotic cells positive for Ki-67 staining, along with a concomitant induction of apoptosis, as indicated by higher expression of cleaved Parp and cleaved caspase 3 (Fig. 6f, g). These functional data suggested that SREBP-mediated lipogenesis is a key downstream effector of PML-loss-driven CaP growth and metastasis. Reference: Nat Genet. 2018 Feb; 50(2): 206–218. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6714980/
Solvent mg/mL mM
Solubility
DMSO 36.5 124.00
Ethanol 75.0 254.74
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 294.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Brovkovych V, Izhar Y, Danes JM, Dubrovskyi O, Sakallioglu IT, Morrow LM, Atilla-Gokcumen GE, Frasor J. Fatostatin induces pro- and anti-apoptotic lipid accumulation in breast cancer. Oncogenesis. 2018 Aug 24;7(8):66. doi: 10.1038/s41389-018-0076-0. PMID: 30140005; PMCID: PMC6107643. 2. Li J, Yan H, Zhao L, Jia W, Yang H, Liu L, Zhou X, Miao P, Sun X, Song S, Zhao X, Liu J, Huang G. Inhibition of SREBP increases gefitinib sensitivity in non-small cell lung cancer cells. Oncotarget. 2016 Aug 9;7(32):52392-52403. doi: 10.18632/oncotarget.10721. PMID: 27447558; PMCID: PMC5239560. 3. Jie Z, Xie Z, Xu W, Zhao X, Jin G, Sun X, Huang B, Tang P, Wang G, Shen S, Qin A, Fan S. SREBP-2 aggravates breast cancer associated osteolysis by promoting osteoclastogenesis and breast cancer metastasis. Biochim Biophys Acta Mol Basis Dis. 2019 Jan;1865(1):115-125. doi: 10.1016/j.bbadis.2018.10.026. Epub 2018 Oct 28. PMID: 30394316. 4. Chen M, Zhang J, Sampieri K, Clohessy JG, Mendez L, Gonzalez-Billalabeitia E, Liu XS, Lee YR, Fung J, Katon JM, Menon AV, Webster KA, Ng C, Palumbieri MD, Diolombi MS, Breitkopf SB, Teruya-Feldstein J, Signoretti S, Bronson RT, Asara JM, Castillo-Martin M, Cordon-Cardo C, Pandolfi PP. An aberrant SREBP-dependent lipogenic program promotes metastatic prostate cancer. Nat Genet. 2018 Feb;50(2):206-218. doi: 10.1038/s41588-017-0027-2. Epub 2018 Jan 15. PMID: 29335545; PMCID: PMC6714980.
In vitro protocol:
1. Brovkovych V, Izhar Y, Danes JM, Dubrovskyi O, Sakallioglu IT, Morrow LM, Atilla-Gokcumen GE, Frasor J. Fatostatin induces pro- and anti-apoptotic lipid accumulation in breast cancer. Oncogenesis. 2018 Aug 24;7(8):66. doi: 10.1038/s41389-018-0076-0. PMID: 30140005; PMCID: PMC6107643. 2. Li J, Yan H, Zhao L, Jia W, Yang H, Liu L, Zhou X, Miao P, Sun X, Song S, Zhao X, Liu J, Huang G. Inhibition of SREBP increases gefitinib sensitivity in non-small cell lung cancer cells. Oncotarget. 2016 Aug 9;7(32):52392-52403. doi: 10.18632/oncotarget.10721. PMID: 27447558; PMCID: PMC5239560.
In vivo protocol:
1. Jie Z, Xie Z, Xu W, Zhao X, Jin G, Sun X, Huang B, Tang P, Wang G, Shen S, Qin A, Fan S. SREBP-2 aggravates breast cancer associated osteolysis by promoting osteoclastogenesis and breast cancer metastasis. Biochim Biophys Acta Mol Basis Dis. 2019 Jan;1865(1):115-125. doi: 10.1016/j.bbadis.2018.10.026. Epub 2018 Oct 28. PMID: 30394316. 2. Chen M, Zhang J, Sampieri K, Clohessy JG, Mendez L, Gonzalez-Billalabeitia E, Liu XS, Lee YR, Fung J, Katon JM, Menon AV, Webster KA, Ng C, Palumbieri MD, Diolombi MS, Breitkopf SB, Teruya-Feldstein J, Signoretti S, Bronson RT, Asara JM, Castillo-Martin M, Cordon-Cardo C, Pandolfi PP. An aberrant SREBP-dependent lipogenic program promotes metastatic prostate cancer. Nat Genet. 2018 Feb;50(2):206-218. doi: 10.1038/s41588-017-0027-2. Epub 2018 Jan 15. PMID: 29335545; PMCID: PMC6714980.
1: Jie Z, Xie Z, Xu W, Zhao X, Jin G, Sun X, Huang B, Tang P, Wang G, Shen S, Qin A, Fan S. SREBP-2 aggravates breast cancer associated osteolysis by promoting osteoclastogenesis and breast cancer metastasis. Biochim Biophys Acta Mol Basis Dis. 2019 Jan;1865(1):115-125. doi: 10.1016/j.bbadis.2018.10.026. Epub 2018 Oct 28. PubMed PMID: 30394316. 2: Pan YX, Zhuo MQ, Li DD, Xu YH, Wu K, Luo Z. SREBP-1 and LXRα pathways mediated Cu-induced hepatic lipid metabolism in zebrafish Danio rerio. Chemosphere. 2019 Jan;215:370-379. doi: 10.1016/j.chemosphere.2018.10.058. Epub 2018 Oct 10. PubMed PMID: 30336314. 3: Brovkovych V, Izhar Y, Danes JM, Dubrovskyi O, Sakallioglu IT, Morrow LM, Atilla-Gokcumen GE, Frasor J. Fatostatin induces pro- and anti-apoptotic lipid accumulation in breast cancer. Oncogenesis. 2018 Aug 24;7(8):66. doi: 10.1038/s41389-018-0076-0. PubMed PMID: 30140005; PubMed Central PMCID: PMC6107643. 4: Chen GH, Luo Z, Hogstrand C, Wu K, Ling SC. SREBP1, PPARG and AMPK pathways mediated the Cu-induced change in intestinal lipogenesis and lipid transport of yellow catfish Pelteobagrus fulvidraco. Food Chem. 2018 Dec 15;269:595-602. doi: 10.1016/j.foodchem.2018.07.048. Epub 2018 Jul 9. PubMed PMID: 30100477. 5: Lo AK, Lung RW, Dawson CW, Young LS, Ko CW, Yeung WW, Kang W, To KF, Lo KW. Activation of sterol regulatory element-binding protein 1 (SREBP1)-mediated lipogenesis by the Epstein-Barr virus-encoded latent membrane protein 1 (LMP1) promotes cell proliferation and progression of nasopharyngeal carcinoma. J Pathol. 2018 Oct;246(2):180-190. doi: 10.1002/path.5130. Epub 2018 Aug 22. PubMed PMID: 29968360; PubMed Central PMCID: PMC6175466. 6: Talebi A, Dehairs J, Rambow F, Rogiers A, Nittner D, Derua R, Vanderhoydonc F, Duarte JAG, Bosisio F, Van den Eynde K, Nys K, Pérez MV, Agostinis P, Waelkens E, Van den Oord J, Fendt SM, Marine JC, Swinnen JV. Sustained SREBP-1-dependent lipogenesis as a key mediator of resistance to BRAF-targeted therapy. Nat Commun. 2018 Jun 27;9(1):2500. doi: 10.1038/s41467-018-04664-0. PubMed PMID: 29950559; PubMed Central PMCID: PMC6021375. 7: Goto A, Ozawa Y, Koda K, Akahori D, Koyauchi T, Amano Y, Kakutani T, Sato Y, Hasegawa H, Matsui T, Yokomura K, Suda T. Clinical impact of minocycline on afatinib-related rash in patients with non-small cell lung cancer harboring epidermal growth factor receptor mutations. Respir Investig. 2018 Mar;56(2):179-183. doi: 10.1016/j.resinv.2017.11.009. Epub 2017 Dec 21. PubMed PMID: 29548657. 8: Gopoju R, Panangipalli S, Kotamraju S. Metformin treatment prevents SREBP2-mediated cholesterol uptake and improves lipid homeostasis during oxidative stress-induced atherosclerosis. Free Radic Biol Med. 2018 Apr;118:85-97. doi: 10.1016/j.freeradbiomed.2018.02.031. Epub 2018 Mar 2. PubMed PMID: 29499335. 9: Gao S, Shi Z, Li X, Li W, Wang Y, Liu Z, Jiang J. Fatostatin suppresses growth and enhances apoptosis by blocking SREBP-regulated metabolic pathways in endometrial carcinoma. Oncol Rep. 2018 Apr;39(4):1919-1929. doi: 10.3892/or.2018.6265. Epub 2018 Feb 13. PubMed PMID: 29436682. 10: Van Krieken R, Marway M, Parthasarathy P, Mehta N, Ingram AJ, Gao B, Krepinsky JC. Inhibition of SREBP With Fatostatin Does Not Attenuate Early Diabetic Nephropathy in Male Mice. Endocrinology. 2018 Mar 1;159(3):1479-1495. doi: 10.1210/en.2018-00093. PubMed PMID: 29420703. 11: Xu Y, Hernández-Ledezma JJ, Hutchison SM, Bogan RL. The liver X receptors and sterol regulatory element binding proteins alter progesterone secretion and are regulated by human chorionic gonadotropin in human luteinized granulosa cells. Mol Cell Endocrinol. 2018 Sep 15;473:124-135. doi: 10.1016/j.mce.2018.01.011. Epub 2018 Jan 31. PubMed PMID: 29366778; PubMed Central PMCID: PMC6045446. 12: Chen M, Zhang J, Sampieri K, Clohessy JG, Mendez L, Gonzalez-Billalabeitia E, Liu XS, Lee YR, Fung J, Katon JM, Menon AV, Webster KA, Ng C, Palumbieri MD, Diolombi MS, Breitkopf SB, Teruya-Feldstein J, Signoretti S, Bronson RT, Asara JM, Castillo-Martin M, Cordon-Cardo C, Pandolfi PP. An aberrant SREBP-dependent lipogenic program promotes metastatic prostate cancer. Nat Genet. 2018 Feb;50(2):206-218. doi: 10.1038/s41588-017-0027-2. Epub 2018 Jan 15. PubMed PMID: 29335545. 13: Merino-Ramos T, Jiménez de Oya N, Saiz JC, Martín-Acebes MA. Antiviral Activity of Nordihydroguaiaretic Acid and Its Derivative Tetra-O-Methyl Nordihydroguaiaretic Acid against West Nile Virus and Zika Virus. Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00376-17. doi: 10.1128/AAC.00376-17. Print 2017 Aug. PubMed PMID: 28507114; PubMed Central PMCID: PMC5527643. 14: Siqingaowa, Sekar S, Gopalakrishnan V, Taghibiglou C. Sterol regulatory element-binding protein 1 inhibitors decrease pancreatic cancer cell viability and proliferation. Biochem Biophys Res Commun. 2017 Jun 17;488(1):136-140. doi: 10.1016/j.bbrc.2017.05.023. Epub 2017 May 5. PubMed PMID: 28483521. 15: Chen GH, Luo Z, Chen F, Shi X, Song YF, You WJ, Liu X. PPARα, PPARγ and SREBP-1 pathways mediated waterborne iron (Fe)-induced reduction in hepatic lipid deposition of javelin goby Synechogobius hasta. Comp Biochem Physiol C Toxicol Pharmacol. 2017 Jul;197:8-18. doi: 10.1016/j.cbpc.2017.04.003. Epub 2017 Apr 11. PubMed PMID: 28411055. 16: Van Krieken R, Chen G, Gao B, Read J, Al Saleh HA, Li R, Al-Nedawi K, Krepinsky JC. Sterol Regulatory Element Binding Protein (SREBP)-1 is a novel regulator of the Transforming Growth Factor (TGF)-β receptor I (TβRI) through exosomal secretion. Cell Signal. 2017 Jan;29:158-167. doi: 10.1016/j.cellsig.2016.11.004. Epub 2016 Nov 5. PubMed PMID: 27826032. 17: Ashikawa Y, Nishimura Y, Okabe S, Sasagawa S, Murakami S, Yuge M, Kawaguchi K, Kawase R, Tanaka T. Activation of Sterol Regulatory Element Binding Factors by Fenofibrate and Gemfibrozil Stimulates Myelination in Zebrafish. Front Pharmacol. 2016 Jul 11;7:206. doi: 10.3389/fphar.2016.00206. eCollection 2016. PubMed PMID: 27462272; PubMed Central PMCID: PMC4939524. 18: Li J, Yan H, Zhao L, Jia W, Yang H, Liu L, Zhou X, Miao P, Sun X, Song S, Zhao X, Liu J, Huang G. Inhibition of SREBP increases gefitinib sensitivity in non-small cell lung cancer cells. Oncotarget. 2016 Aug 9;7(32):52392-52403. doi: 10.18632/oncotarget.10721. PubMed PMID: 27447558; PubMed Central PMCID: PMC5239560. 19: Mustafa M, Wang TN, Chen X, Gao B, Krepinsky JC. SREBP inhibition ameliorates renal injury after unilateral ureteral obstruction. Am J Physiol Renal Physiol. 2016 Sep 1;311(3):F614-25. doi: 10.1152/ajprenal.00140.2016. Epub 2016 Jul 6. PubMed PMID: 27385736. 20: Gholkar AA, Cheung K, Williams KJ, Lo YC, Hamideh SA, Nnebe C, Khuu C, Bensinger SJ, Torres JZ. Fatostatin Inhibits Cancer Cell Proliferation by Affecting Mitotic Microtubule Spindle Assembly and Cell Division. J Biol Chem. 2016 Aug 12;291(33):17001-8. doi: 10.1074/jbc.C116.737346. Epub 2016 Jul 4. PubMed PMID: 27378817; PubMed Central PMCID: PMC5016105.