ST1072
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity : 97.30%
- CAS No.: 1402703-50-7
- Formula: C28H41NO4
- Molecular Weight:455.63
-
Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[3]|
PKCθ |
N-Ras |
In Vitro
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 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.
-
Cell Line:HCT-116 human colon cancer cells
-
Concentration:0-80 μM
-
Incubation Time:48 h
-
Result:Reduced HCT-116 cell viability in a concentration-dependent manner.
Reduced viability starting at 20 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c (recipient, lethally irradiated, MHC-mismatched allogeneic bone marrow transplantation model); C57BL/6 (donor, wild-type)[3]
-
Dosage:2 mg/kg
-
Administration:i.p.; daily; day -1 to day 28 post-transplant
-
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.
-
Animal Model:BALB/c (recipient, lethally irradiated, MHC-mismatched allogeneic bone marrow transplantation model with mixed-lineage leukemia); C57BL/6 (donor)[3]
-
Dosage:1 mg/kg
-
Administration:i.p.; daily; day -1 to day 14 post-transplant
-
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.
-
Animal Model:BALB/c (recipient, lethally irradiated, MHC-mismatched allogeneic bone marrow transplantation model); C57BL/6 (donor, β-actin luciferase transgenic)[3]
-
Dosage:1 mg/kg
-
Administration:i.p.; daily; day -1 to day 14 post-transplant
-
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
-
CAS No. 1402703-50-7
-
Appearance Solid
-
Molecular Weight 455.63
-
Formula C28H41NO4
-
Color White to off-white
-
SMILES
O=C(CCCC1=CC=CC=C1)NC(CO)(CCC2=CC=C(C=C2)OCCCCCCC)CO
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (219.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.49 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1948 mL | 10.9738 mL | 21.9476 mL | 54.8691 mL |
| 5 mM | 0.4390 mL | 2.1948 mL | 4.3895 mL | 10.9738 mL | |
| 10 mM | 0.2195 mL | 1.0974 mL | 2.1948 mL | 5.4869 mL | |
| 15 mM | 0.1463 mL | 0.7316 mL | 1.4632 mL | 3.6579 mL | |
| 20 mM | 0.1097 mL | 0.5487 mL | 1.0974 mL | 2.7435 mL | |
| 25 mM | 0.0878 mL | 0.4390 mL | 0.8779 mL | 2.1948 mL | |
| 30 mM | 0.0732 mL | 0.3658 mL | 0.7316 mL | 1.8290 mL | |
| 40 mM | 0.0549 mL | 0.2743 mL | 0.5487 mL | 1.3717 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4390 mL | 1.0974 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.9145 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2743 mL | 0.6859 mL | |
| 100 mM | 0.0219 mL | 0.1097 mL | 0.2195 mL | 0.5487 mL |
ST1072 Related Classifications
HY-133488 Related Classifications
Powered by Bioz