SRSF1-IN-1
SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma.
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- 화학식: C20H24O5S
- 분자량:376.47
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
제품 설명
In Vitro
SRSF1-IN-1 (STP2) (72 h) potently inhibits the proliferation of HepG2, MCF7, HCT116, U251, HGC27, AGS, BGC823, SGC7901, A549 and B16F10 cell lines, with IC50 values of 0.63, 1.79, 0.52, 2.43, 0.62, 1.03, 1.3, 1.88, >10 and 1.03 μM, respectively. It also exhibits selective toxicity toward tumor cells compared with normal human LO2 hepatocytes[1].
SRSF1-IN-1 (0.5-2 μM; 48 h) induces dose-dependent apoptosis in HGC27 and AGS gastric cancer cells, increases the proportion of apoptotic cells, downregulates the anti-apoptotic protein Bcl-xl, and upregulates cleaved PARP and cleaved caspase 3[1].
SRSF1-IN-1 (0.5-2 μM; 24 h) arrests HGC27 and AGS gastric cancer cells at the S phase, accompanied by upregulated expression of the P21 protein and downregulated expression of the CyclinE2 protein[1].
SRSF1-IN-1 (0.5-2 μM; 24 h) downregulates SRSF1 mRNA and protein expression in a dose-dependent manner in HGC27 and AGS gastric cancer cells; at the concentration of 2 μM, it inhibits the RNA splicing pathway in HGC27 cells and upregulates autophagy-related genes[1].
SRSF1-IN-1 (0.5-2 μM; 48 h) induces autophagy in HGC27 and AGS gastric cancer cells; when combined with 2 μM Chloroquine (CQ) (HY-17589A) for 24 h, it also enhances the formation of LC3B puncta[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HGC27, AGS
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a dose-dependent manner: in HGC27 cells, apoptosis proportion increased from 8.15% to 47.8%; in AGS cells, apoptosis proportion increased from 7.59% to 63.3%.
Reduced anti-apoptotic Bcl-xl protein expression and increased cleaved-PARP and cleaved-caspase 3 expression in both cell lines.
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Cell Line:HGC27, AGS
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Increased the proportion of S-phase cells: in HGC27 cells, S-phase proportion rose from 50.19% to 75.34%; in AGS cells, S-phase proportion rose from 32.86% to 52.16%.
Increased P21 protein expression and reduced CyclinE2 protein expression in both cell lines, with no obvious dose dependence.
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Cell Line:HGC27, AGS
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Showed significant downregulation of the RNA splicing pathway, reduced mRNA expression of SRSF1, and increased expression of autophagy-related genes (BECN1, MAP1LC3B, MAP1LC3B2) in HGC27 cells treated with 2 μM.
Confirmed dose-dependent reduction of SRSF1 mRNA levels in both HGC27 and AGS cells.
Showed corresponding dose-dependent reduction of SRSF1 protein levels in both cell lines.
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Cell Line:HGC27, AGS
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:48 h (Western blot); 24 h (immunofluorescence)
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Result:Increased ATG5, Beclin1, and LC3 II/LC3 I ratio, and decreased P62 protein levels in both HGC27 and AGS cells at 0.5, 1, and 2 μM for 48 h.
Resulted in a significant increase in LC3B puncta in HGC27 cells when combined with CQ (20 μM) for 24 h at 2 μM.
In Vivo
STP2 (1 g/kg; i.p.; single dose) is well-tolerated in male ICR mice, with 100% survival, gradual weight gain, and no apparent liver histopathological abnormalities over 7 days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6 weeks old, gastric cancer xenograft model with HGC27 cells)[1]
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Dosage:25 mg/kg; 100 mg/kg
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Administration:i.p.; daily; 15 days
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Result:Suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition (TGI) values of 63.68% at 25 mg/kg and 82.66% at 100 mg/kg.
Caused no apparent body weight loss during the 15-day treatment period.
Reduced P62 protein levels and increased LC3B protein levels (a marker of autophagy) in HGC27 tumor tissues from treated mice.
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Animal Model:ICR (male)[1]
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Dosage:1 g/kg
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Administration:i.p.; single dose
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Result:Resulted in 100% survival of mice over the 7-day observation period.
Led to gradual weight gain in mice over the 7-day duration.
Caused no obvious abnormal changes in hepatocyte morphology in liver tissues, with no enlarged volume, empty/bright cytoplasm, or unclear cell boundaries observed.
Chemical Information
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분자량 376.47
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화학식 C20H24O5S
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SMILES
S=C1OCC2=C1CC[C@@]3(C)[C@@]2([H])C[C@H](O4)[C@]54[C@@]3(O6)[C@@H]6[C@H]7[C@@](O7)(C(C)C)[C@H]5O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SRSF1-IN-1 Related Classifications
HY-170935 Related Classifications
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