P-SiaFNEtoc
P-SiaFNEtoc is a Sialyltransferase inhibitor that blocks sialic acid capping of glycans. P-SiaFNEtoc forms CMP-SiaFNEtoc, reduces endogenous CMP-Neu5Ac, feedback-inhibits GNE, and depletes sialylation on N-glycans and O-GalNAc glycans. P-SiaFNEtoc decreases cell surface sialoglycan levels, VEGF and DKK-1 secretion, Tn antigen levels, and cell cycle checkpoint/E2F target gene expression, while inducing p27/Kip1 and fucosylation. P-SiaFNEtoc can be used in research on prostate cancer, and melanoma.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 3138013-03-0
- 화학식: C23H32FNO15
- 분자량:581.50
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
사이즈
가격
재고
수량
Amount: USD 0.00
Please select quantity
or
or
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocol
- 순도&문서
- References
-
Help & FAQs
All VEGFR Isoforms
More
Biological Activity
제품 설명
P-SiaFNEtoc is a Sialyltransferase inhibitor that blocks sialic acid capping of glycans. P-SiaFNEtoc forms CMP-SiaFNEtoc, reduces endogenous CMP-Neu5Ac, feedback-inhibits GNE, and depletes sialylation on N-glycans and O-GalNAc glycans. P-SiaFNEtoc decreases cell surface sialoglycan levels, VEGF and DKK-1 secretion, Tn antigen levels, and cell cycle checkpoint/E2F target gene expression, while inducing p27/Kip1 and fucosylation. P-SiaFNEtoc can be used in research on prostate cancer, and melanoma[1][2][3][4][5].
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
0.3964 μM
|
Inhibition of global sialylation in human PC3 prostate cancer cells by P-SiaFNEtoc assessed by Pan-sialic acid Lectenz flow cytometry after 3-day incubation.
Inhibition of global sialylation in human PC3 prostate cancer cells by P-SiaFNEtoc assessed by Pan-sialic acid Lectenz flow cytometry after 3-day incubation.
|
37847613 |
| THP-1 | EC50 |
0.27 μM
|
Inhibition of sialylation in human THP-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human THP-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| HEK293 | EC50 |
0.90 μM
|
Inhibition of sialylation in human HEK293 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human HEK293 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| SH-SY5Y | EC50 |
1.96 μM
|
Inhibition of sialylation in human SH-SY5Y cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human SH-SY5Y cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| MC-38 | EC50 |
41.30 μM
|
Inhibition of sialylation in murine MC38 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in murine MC38 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| A549 | EC50 |
2.20 μM
|
Inhibition of sialylation in human A549 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human A549 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| NCI-H1299 | EC50 |
0.35 μM
|
Inhibition of sialylation in human H1299 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human H1299 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| MDA-MB-231 | EC50 |
0.96 μM
|
Inhibition of sialylation in human MDA-MB-231 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human MDA-MB-231 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| SK-OV-3 | EC50 |
1.10 μM
|
Inhibition of sialylation in human SKOV-3 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human SKOV-3 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| IGROV-1 | EC50 |
0.73 μM
|
Inhibition of sialylation in human IGROV-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human IGROV-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| OVCAR-3 | EC50 |
0.58 μM
|
Inhibition of sialylation in human OVCAR-3 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human OVCAR-3 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| PANC-1 | EC50 |
0.80 μM
|
Inhibition of sialylation in human PANC-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human PANC-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
| CAPAN-1 | EC50 |
6.60 μM
|
Inhibition of sialylation in human Capan-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
Inhibition of sialylation in human Capan-1 cells assessed as reduction of Pan-Lectenz binding after 3 days by flow cytometry.
|
41190337 |
In Vitro
Anti-cancerCell Cycle RegulationInnate ImmunityCarbohydrate Metabolism
Anti-cancer
P-SiaFNEtoc (64 µM; 72 h) inhibits α2,6 sialylation in TRAMPC2 murine prostate cancer cells without reducing viability[1].
P-SiaFNEtoc (256 µM; 72 h) inhibits sialylation in RM1 murine prostate cancer cells[1].
P-SiaFNEtoc (0.01-4 µM; 3 days) inhibits global sialylation in PC3 and CWR22RV1 prostate cancer cells with IC50 values of 0.3964 µM and 0.08700 µM, respectively[2].
P-SiaFNEtoc (2 µM; 72 h) reduces α2-6- and α2-3-linked sialylated glycans in PC3 and CWR22RV1 prostate cancer cells[2].
P-SiaFNEtoc (20 µM; 6 days) suppresses SNA lectin-detected α2,6-sialylation in both VCaP and VCaPEnzR prostate cancer cells[5].
P-SiaFNEtoc (2 µM; 3 days) reduces SNA lectin-detected α2,6-sialylation in both LNCaP and LNCaPEnzR prostate cancer cells[5].
P-SiaFNEtoc (20 µM; 6 days) combined with Enzalutamide (HY-70002) partially reverses acquired enzalutamide resistance in VCaPEnzR cells, producing a 38.33% IC50 reversion and an IC50 of 19.10 µM[5].
P-SiaFNEtoc (256 µM; 72 h) inhibits sialylation in RM1 murine prostate cancer cells[1].
P-SiaFNEtoc (0.01-4 µM; 3 days) inhibits global sialylation in PC3 and CWR22RV1 prostate cancer cells with IC50 values of 0.3964 µM and 0.08700 µM, respectively[2].
P-SiaFNEtoc (2 µM; 72 h) reduces α2-6- and α2-3-linked sialylated glycans in PC3 and CWR22RV1 prostate cancer cells[2].
P-SiaFNEtoc (20 µM; 6 days) suppresses SNA lectin-detected α2,6-sialylation in both VCaP and VCaPEnzR prostate cancer cells[5].
P-SiaFNEtoc (2 µM; 3 days) reduces SNA lectin-detected α2,6-sialylation in both LNCaP and LNCaPEnzR prostate cancer cells[5].
P-SiaFNEtoc (20 µM; 6 days) combined with Enzalutamide (HY-70002) partially reverses acquired enzalutamide resistance in VCaPEnzR cells, producing a 38.33% IC50 reversion and an IC50 of 19.10 µM[5].
Anti-cancer
Cell Cycle Regulation
P-SiaFNEtoc (2 µM; 72 h) increases p27/Kip1 expression in CWR22RV1 prostate cancer cells[2].
Innate Immunity
Carbohydrate Metabolism
P-SiaFNEtoc (128-200 μM; 3-6 days) dose-dependently inhibits sialylation in most mammalian cell lines, with an EC90 of 1.08 μM in THP-1, but RAW 264.7 is insensitive[3].
P-SiaFNEtoc produced 20-60% sialylation inhibition in primary human macrophages[3].
P-SiaFNEtoc produced 20-60% sialylation inhibition in primary human macrophages[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Immunofluorescence[2]
-
Cell Line:PC3 and CWR22RV1 prostate cancer cells
-
Concentration:2 µM
-
Incubation Time:72 h
-
Result:Reduced SNA staining for α2-6-linked sialic acid and reduced MAL-I staining for α2-3-linked sialic acid occurred in both PC3 and CWR22RV1 cells.
Immunofluorescence[2]
-
Cell Line:CWR22RV1 prostate cancer cells
-
Concentration:2 µM
-
Incubation Time:72 h
-
Result:p27/Kip1 protein levels were increased in CWR22RV1 cells by immunocytochemistry and CTCF quantification.
Immunofluorescence[5]
-
Cell Line:VCaP and VCaPEnzR prostate cancer cells
-
Concentration:20 µM
-
Incubation Time:6 days
-
Result:SNA lectin recognition was suppressed in both VCaP control and VCaPEnzR cells, indicating a reduction in α2,6-sialylated N-glycans.
Cell Viability Assay[5]
-
Cell Line:VCaP and VCaPEnzR prostate cancer cells
-
Concentration:20 µM (with enzalutamide concentration series)
-
Incubation Time:6 days (144 h)
-
Result:Co-incubation with enzalutamide resulted in IC50 values of 8.30 µM for VCaP cells and 19.10 µM for VCaPEnzR cells.
In VCaPEnzR cells, a 38.33% IC50 reversion occurred compared with enzalutamide alone; the VCaP control IC50 was not altered.
In Vivo
Anti-cancer
P-SiaFNEtoc (64 μM; in vitro preincubation; single; 72 h) reduces subcutaneous tumour burden in immunocompetent C57BL/6 mice following preincubation of TRAMPC2 prostate cancer cells[1].
P-SiaFNEtoc (256 μM; in vitro preincubation; single; 72 h) reduces skeletal tumour burden and bone destruction and prolongs survival in immunocompetent C57BL/6 mice following preincubation of RM1 prostate cancer cells[1].
P-SiaFNEtoc (256 μM; in vitro preincubation; single; 72 h) reduces skeletal tumour burden and bone destruction and prolongs survival in immunocompetent C57BL/6 mice following preincubation of RM1 prostate cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (RRID:MGI:2159769; male; 6 weeks old)[1]
-
Dosage:64 μM
-
Administration:in vitro preincubation; single; 72 h
-
Result:Overt tumour burden was reduced in mice receiving preincubated TRAMPC2 cells compared with vehicle-preincubated cells (n=10 per group).
-
Animal Model:C57BL/6 (RRID:MGI:2159769; male; 6 weeks old)[1]
-
Dosage:256 μM
-
Administration:in vitro preincubation; single; 72 h
-
Result:Formed fewer skeletal tumours per mouse and had lower long-bone tumour incidence than vehicle-preincubated cells; survival was prolonged.
Ex vivo micro-CT showed increased trabecular bone volume fraction (BV/TV) by 63% and trabecular number (Tb.N) by 51% (n=9 per group).
Chemical Information
-
CAS No. 3138013-03-0
-
분자량 581.50
-
화학식 C23H32FNO15
-
SMILES
COC(C1(O[C@@]([C@@H]([C@H]([C@H]1F)OC(C)=O)NC(OCC)=O)([H])[C@H](OC(C)=O)[C@H](OC(C)=O)COC(C)=O)OC(C)=O)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
References
Calculators
몰농도 계산기
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
=
×
×
농도 희석 계산기
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P-SiaFNEtoc Related Classifications
HY-188400 Related Classifications
Powered by Bioz