2. Cell Cycle/DNA Damage Epigenetics Apoptosis Autophagy
  3. SRPK PARP Caspase Apoptosis Autophagy
  4. 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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SRSF1-IN-1

SRSF1-IN-1 Chemical Structure

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SRSF1-IN-1 Related Antibodies

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Description

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[1].

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.

SRSF1-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HGC27, AGS
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
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.

Cell Cycle Analysis[1]

Cell Line: HGC27, AGS
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
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.

Real Time qPCR[1]

Cell Line: HGC27, AGS
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
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.

Cell Autophagy Assay[1]

Cell Line: HGC27, AGS
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h (Western blot); 24 h (immunofluorescence)
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 (25-100 mg/kg; i.p.; daily; 15 days) exhibits dose-dependent in vivo antitumor activity in a mouse HGC27 gastric cancer xenograft model, with 63.68% and 82.66% tumor growth inhibition at doses of 25 mg/kg and 100 mg/kg, respectively, without causing apparent body weight loss[1].
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.

Animal Model: BALB/c nude (male, 6 weeks old, gastric cancer xenograft model with HGC27 cells)[1]
Dosage: 25 mg/kg; 100 mg/kg
Administration: i.p.; daily; 15 days
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.
Animal Model: ICR (male)[1]
Dosage: 1 g/kg
Administration: i.p.; single dose
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.
Molecular Weight

376.47

Formula

C20H24O5S
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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SRSF1-IN-1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SRSF1-IN-1SRPKPARPCaspaseApoptosisAutophagySerine-arginine protein kinasespoly ADP ribose polymerase apoptosisHepG2 cellsMCF7 cellsHCT116 cellsU251 cellsHGC27 cellsAGS cellsBGC823 cellsSGC7901 cellsA549 cellsB16F10 cellsautophagyBALB/c nude miceICR miceiver cancergastric cancerbreast cancercolon cancergliomamelanomaInhibitorinhibitorinhibit

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