ST1072
ST1072 is an inhibitor of CerS4 and CerS6. ST1072 preferentially inhibits CerS6 over CerS4, and reduces the production of C16 ceramide. ST1072 impairs TCR-mediated N-RAS activation, ERK signaling pathway, and the colocalization of CD3/PKCθ. ST1072 decreases the production of IFN-γ as well as the migration of donor cells to target organs. ST1072 regulates immune cell populations and the expression of co-stimulatory molecules. ST1072 can be used in research related to colon cancer, cervical cancer, graft-versus-host disease, and hematologic malignancies.
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- CAS No.: 1402703-50-7
- Formule: C28H41NO4
- Masse moléculaire:455.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PKCθ |
N-Ras |
ST1072 (10 min preincubation, 30 min reaction) potently inhibits ceramide synthase activity in HCT-116 cell microsomes, with the highest potency against C18:0-dhCer synthesis (IC50 = 26.9 μM) followed by C16:0-dhCer (IC50 = 50.4 μM) and weaker activity against C24:0-dhCer (IC50 = 81.3 μM)[1].
ST1072 (0-80 μM; 48 h) reduces the viability of HCT-116 human colon cancer cells in a concentration-dependent manner starting at 20 μM after 48 h of incubation[1].
ST1072 (25 μM) significantly reduces C16:0-dhCer, C24:0-dhCer, and C24:1-dhCer levels in HeLa human cervical cancer cells after 48 h of incubation[1].
ST1072 (5-30 μM; 48 h) potently reduces ceramide levels in HeLa human cervical cancer cells, with the highest potency against C16:0-Cer (IC50 = 6.8 μM) followed by C14:0-Cer (IC50 = 12.2 μM) and C24:1-Cer (IC50 = 14.5 μM) after 48 h of incubation[1].
ST1072 (50 μM; 5 days) potently inhibits allogeneic proliferation and IFN-γ production in primary murine WT T cells[2].
ST1072 (50 μg/mL; 24 h-5 days) inhibits TCR-mediated N-RAS activation and downstream ERK signaling in primary mouse wild-type T cells, reducing IFN-γ production in CD4 T cells, an effect reversed by active N-RAS overexpression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 human colon cancer cells
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Concentration:0-80 μM
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Incubation Time:48 h
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Result:Reduced HCT-116 cell viability in a concentration-dependent manner.
Reduced viability starting at 20 μM.
ST1072 (1 mg/kg; i.p.; daily; day -1 to day 14 post-transplant) significantly reduces acute GVHD severity and improves survival while preserving the GVL effect against mixed-lineage leukemia in an MHC-mismatched murine allogeneic bone marrow transplantation model[3].
ST1072 (1 mg/kg; i.p.; daily; day -1 to day 14 post-transplant) significantly reduces donor T-cell expansion and migration to GVHD target organs in an MHC-mismatched murine allogeneic bone marrow transplantation model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (recipient, lethally irradiated, MHC-mismatched allogeneic bone marrow transplantation model); C57BL/6 (donor, wild-type)[3]
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Dosage:2 mg/kg
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Administration:i.p.; daily; day -1 to day 28 post-transplant
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Result:Significantly reduced cGVHD severity, reflected by reduced body weight loss and lower clinical scores.
Matched cGVHD severity of recipients transplanted with CerS6 knockout donor grafts.
Selectively reduced serum levels of C16 ceramide compared to vehicle controls.
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Animal Model:BALB/c (recipient, lethally irradiated, MHC-mismatched allogeneic bone marrow transplantation model with mixed-lineage leukemia); C57BL/6 (donor)[3]
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Dosage:1 mg/kg
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Administration:i.p.; daily; day -1 to day 14 post-transplant
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Result:Significantly reduced aGVHD clinical scores compared to vehicle controls.
Improved recipient survival compared to vehicle controls.
Preserved the GVL effect: recipients treated were free from MLL, while most vehicle-treated recipients died from aGVHD.
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Animal Model:BALB/c (recipient, lethally irradiated, MHC-mismatched allogeneic bone marrow transplantation model); C57BL/6 (donor, β-actin luciferase transgenic)[3]
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Dosage:1 mg/kg
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Administration:i.p.; daily; day -1 to day 14 post-transplant
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Result:Significantly reduced bioluminescent signal intensity in recipient spleens, lungs, and guts compared to vehicle controls, indicating reduced donor T-cell expansion and migration to these sites.
Increased absolute numbers of donor CD4 and CD8 T cells in recipient spleens but decreased them in recipient livers.
Reduced expression of CXCR3, CCR5, CCR6, and CCR9 on donor T cells in spleens.
Chemical Information
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CAS No. 1402703-50-7
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Masse moléculaire 455.63
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Formule C28H41NO4
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SMILES
O=C(CCCC1=CC=CC=C1)NC(CO)(CCC2=CC=C(C=C2)OCCCCCCC)CO
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Schiffmann S, et al. Inhibitors of specific ceramide synthases. Biochimie. 2012 Feb;94(2):558-65. [Content Brief]
[2]. Sofi MH, et al. Ceramide synthesis regulates T cell activity and GVHD development. JCI insight. 2017 May 18;2(10):e91701. [Content Brief]
[3]. Sofi MH, et al. Ceramide synthase 6 impacts T-cell allogeneic response and graft-versus-host disease through regulating N-RAS/ERK pathway. Leukemia. 2022 Jul;36(7):1907-1915. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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