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Chemical Structure| 125256-00-0 Chemical Structure| 125256-00-0

Structure of Fatostatin
CAS No.: 125256-00-0

Chemical Structure| 125256-00-0

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Fatostatin (125B11) is a specific inhibitor of SREBP activation, impeding the activation of SREBP-1 and SREBP-2. It binds to SCAP (SREBP cleavage-activating protein) and inhibits the ER-Golgi translocation of SREBPs, decreasing the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties and lowers hyperglycemia in ob/ob mice.

Synonyms: 125B11

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Product Details of Fatostatin

CAS No. :125256-00-0
Formula : C18H18N2S
M.W : 294.41
SMILES Code : CC1=CC=C(C2=CSC(C3=CC(CCC)=NC=C3)=N2)C=C1
Synonyms :
125B11
MDL No. :MFCD02376000
InChI Key :ZROSUBKIGBSZCG-UHFFFAOYSA-N
Pubchem ID :1889993

Safety of Fatostatin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RS4;11 and ALL-PO cells 1 μM 48 h Sequential administration of AZD1775 in conjunction with several of these drugs effectively inhibited the recovery of RS4;11 and ALL-PO cells. PMC11143599
U87R cells 3.93 µM 5 days To test the inhibitory effect of Fatostatin on TMZ-resistant cells, the results showed that the IC50 of Fatostatin for U87R cells was 3.93 µM, significantly lower than the IC50 of TMZ. PMC9958008
U87 cells 8.69 µM 5 days To test the inhibitory effect of Fatostatin on TMZ-sensitive cells, the results showed that the IC50 of Fatostatin for U87 cells was 8.69 µM. PMC9958008
RD cells 0.01 - 1 µM 48 hours inhibited cell growth and migration PMC11750561
RH30 cells 0.01 - 1 µM 48 hours inhibited cell growth and migration PMC11750561
RD cells 1 mM 48 hours increased cell death PMC11750561
MCF-7 cells 5 μM 48 hours Fatostatin inhibited the growth of ER+ cells, leading to cell cycle arrest and apoptosis. PMC6107643
T47D cells 5 μM 48 hours Fatostatin inhibited the growth of ER+ cells, leading to cell cycle arrest and apoptosis. PMC6107643
MDA-MB-231 cells 5 μM 48 hours Fatostatin had no significant effect on the growth of ER- cells. PMC6107643
BT20 cells 5 μM 48 hours Fatostatin had no significant effect on the growth of ER- cells. PMC6107643

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Patient-derived xenograft (PDX) model Intravenous injection 120 mg/kg 5 days a week for 21 days To assess the in vivo efficacy of AZD1775 in treating ALL; results indicated effectiveness in the PDX model. PMC11143599
Mice Subcutaneous C4-2B xenograft mouse model Intraperitoneal injection 15 mg/kg 42 days Fatostatin significantly reduced tumor growth and serum PSA levels. PMC4084917
Mice Ptenpc−/−; Pmlpc−/− mouse model Intraperitoneal (i.p.) injections 15 mg/kg Every other day for 2 months Fatostatin inhibited both prostate tumor growth and distant lymph node metastasis, significantly reduced the expression of SREBP-regulated enzymes for synthesis of FA and cholesterol, decreased the frequency of Ki-67 positive cells, and induced apoptosis. PMC6714980
NOD/SCID mice RD cell xenograft model Oral 10 mg/kg 3 times a week for 3 weeks reduced tumor growth PMC11750561
Mice MCF-7 cell xenograft model Intraperitoneal injection 30 mg/kg/day Once daily for 16 days Fatostatin significantly reduced the growth of MCF-7 xenograft tumors and induced endoplasmic reticulum stress and apoptosis. PMC6107643

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.40mL

0.68mL

0.34mL

16.98mL

3.40mL

1.70mL

33.97mL

6.79mL

3.40mL

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