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Chemical Structure| 298197-04-3 Chemical Structure| 298197-04-3

Structure of Fatostatin HBr
CAS No.: 298197-04-3

Chemical Structure| 298197-04-3

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Fatostatin hydrobromide (125B11 hydrobromide) specifically inhibits SREBP activation, impeding SREBP-1 and SREBP-2 activation. It binds to SCAP (SREBP cleavage-activating protein) and prevents the ER-Golgi translocation of SREBPs, decreasing the transcription of lipogenic genes in cells. Fatostatin hydrobromide exhibits antitumor properties and reduces hyperglycemia in ob/ob mice.

Synonyms: 125B11 hydrobromide; Fatostatin hydrobromide; 125B11

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Product Details of Fatostatin HBr

CAS No. :298197-04-3
Formula : C18H19BrN2S
M.W : 375.33
SMILES Code : CC1=CC=C(C2=CSC(C3=CC(CCC)=NC=C3)=N2)C=C1.[H]Br
Synonyms :
125B11 hydrobromide; Fatostatin hydrobromide; 125B11
MDL No. :MFCD02376000
InChI Key :RJCFNQZVFUMORB-UHFFFAOYSA-N
Pubchem ID :2850562

Safety of Fatostatin HBr

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
A549 cells 2 μM 24 hours Inhibits SREBP2 activation, reduces LD accumulation, and decreases viral replication and inflaμMatory response. PMC11873989
RD cells 0.01 e1 μM 48 hours impaired cell growth and migration PMC11750561
RH30 cells 0.01 e1 μM 48 hours impaired cell growth and migration PMC11750561
RD cells 5 e50 μM 48 hours promoted oxidative cell death and chemosensitization PMC11750561
RH30 cells 5 e50 μM 48 hours promoted oxidative cell death and chemosensitization PMC11750561
Chinese hamster ovary-K1 cells (CHO-K1) 5.6 μM Inhibited SREBP activation, reduced reporter gene activity PMC3136361
HK1 cells 15 μM 16 hours To investigate the effect of Fatostatin on LMP1-induced lipogenesis, results showed that Fatostatin significantly inhibited lipogenesis PMC6175466

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Pten and Pml double-null prostate cancer model Intraperitoneal injection 37.5–300 mg/kg twice daily for 21 days To evaluate the inhibitory effect of Fatostatin on tumor growth and metastasis, results showed that Fatostatin significantly inhibited tumor growth and lymph node metastasis PMC6714980
mice Ptenpc−/−; Pmlpc−/− mice intraperitoneal (i.p.) injections single injection, monitored for 36 days Fatostatin inhibited both prostate tumor growth and distant lymph node metastasis, presumably due to the suppression of the SREBP pathway, as fatostatin-treated tumors displayed markedly lower expression of FA and cholesterol synthesis enzymes. PMC6714980
Mice BALB/c mice Intraperitoneal injection 15 mg/kg Every other day for 2 months Improves survival rate of infected mice, alleviates lung injury, and inhibits viral replication and inflammatory response. PMC11873989
ICR mice Unilateral ureteral obstruction (UUO) model Intraperitoneal injection 15 mg/kg every other day for 2 months Fatostatin inhibited the AA-induced increase in nSREBP-1 expression and reduced the level of 15d-PGJ2, indicating that Fatostatin reduces the generation of 15d-PGJ2 by inhibiting SREBP-1 activity. PMC7471452
NOD/SCID mice RD cell xenograft model oral 5, 10, 20, 30 mg/kg Three times, two days before infection, on the day of infection, and two days after infection reduced tumor mass PMC11750561
Mice Obese ob/ob mice Oral 30 mg·kg−1 per day Once a day for 3 days Inhibited weight gain, blood glucose, and hepatic fat accumulation, ameliorated fatty liver conditions PMC3136361
Nude mice C666-1 xenograft model Intraperitoneal injection Approximately 0.7 mg/day, approximately 23 mg/kg body weight 8 weeks To investigate the inhibitory effect of Fatostatin on NPC tumor growth, results showed that Fatostatin significantly inhibited tumor growth PMC6175466

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.64mL

5.33mL

2.66mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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