CT 32228
Based on 1 Customer Validation
CT 32228 is a selective LPAAT-β inhibitor with an IC50 of 60 nM. CT 32228 inhibits LPAAT-β-mediated acyl-CoA-dependent acylation of lysophosphatidic acid and lysophosphatidylmethanol in a non-competitive and isoform-specific manner, reducing phosphatidic acid and downstream oncogenic signaling. CT 32228 exerts antiproliferative and cytotoxic activity in tumor cell lines and multiple myeloma cells, inducing caspase-mediated apoptosis and cell cycle arrest. CT 32228 can be used for research on multiple myeloma, non-Hodgkin's lymphoma, and acute leukemia.
For research use only. We do not sell to patients.
- Purity : 95.27%
- CAS No.: 521064-34-6
- Formula: C16H13BrClN5
- Molecular Weight:390.66
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[2]|
LPAAT-β 60 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| K562 | IC50 |
0.4 μM
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Antiproliferative activity against human K562 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human K562 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
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16488473 |
| U-937 | IC50 |
0.2 μM
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Antiproliferative activity against human U937 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human U937 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
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16488473 |
| MOLT-4 | IC50 |
0.1 μM
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Antiproliferative activity against human Molt4 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human Molt4 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
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16488473 |
| HL-60 | IC50 |
0.1 μM
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Antiproliferative activity against human HL60 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human HL60 leukemia cells assessed as viability reduction incubated 72 hrs by MTT assay.
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16488473 |
In Vitro
CT-32228 inhibits the proliferation of Ramos, FL-18, and DHL-4 lymphoma cells, with an IC50 of 50-100 nM at 24 hours and maximal inhibition at 500 nM[4].
CT-32228 (72 hours) inhibits the growth of CEM, K562, U937, Molt4, AML193, and HL60 leukemia cell lines, with IC50 values of 0.1 to 0.8 µM[5].
CT-32228 (50 nM; 48 hours) induces Annexin V apoptosis in DHL-4 and Ramos lymphoma cells, and its combination with Rituximab (HY-P9913) increases apoptosis[4].
CT-32228 (50 nM; 48 hours) activates caspases in DHL-4 and Ramos lymphoma cells, and when combined with Rituximab, induces caspase-positive apoptosis in 26.2% and 21.2% of the cells, respectively[4].
CT-32228 (2 µM; 48 hours) induces significant apoptosis in CEM cells[5].
CT-32228 (2 µM; 48 hours) induces more apoptosis in undifferentiated U937 cells than in PMA-differentiated U937 cells[5].
CT-32228 (10 µM) reduces acylation of lysoPM by approximately 50% in the control group and by 60-75% in LPAAT-β-overexpressing PC-3 whole cells[1].
CT-32228 inhibits whole-cell PM formation in PC-3/b1 cells overexpressing LPAAT-β (IC50 values of 321, 353, and 1,940 nM, respectively) and in DU145 cells transduced with LPAAT-β (IC50 900 nM)[1].
CT-32228 (compound 1) inhibits LPAAT-b with an IC50 of 0.06 μM[2].
CT-32228 inhibits an average of 57% of LPAAT activity in normal lymphocyte lysates[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ramos human Burkitt’s lymphoma cells
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Concentration:50, 100, 200, 400, 800 nM
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Incubation Time:48 h
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Result:Produced minimal apoptosis below 100 nM.
Induced Annexin V positivity at higher concentrations, with ~50% Annexin V-positive cells at 200-800 nM.
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Cell Line:CEM human leukemia cells
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Concentration:2 µM
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Incubation Time:48 h
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Result:The Annexin V-positive/PI-positive population (R2) was 93.12% and the Annexin V-negative/PI-negative population (R3) was 2.46%.
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Cell Line:U937 human leukemia cells with or without PMA-induced differentiation
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Concentration:2 µM
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Incubation Time:48 h
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Result:Significantly induced apoptosis.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD CB17 SCID (6-8 weeks old)[4]
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Dosage:72 mg/kg (monotherapy); 72 mg/kg with Rituximab 10 mg/kg (combination)
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Administration:i.p.; daily for 5 days/week for 4 weeks (20 total doses); Rituximab i.p.; weekly for 4 weeks (4 doses)
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Result:Five of five (100%) mice developed palpable tumors by day 16 after tumor implantation; all five were euthanized by day 31 because of significant wasting despite the absence of tumor progression.
With Rituximab, no tumor development was detected in any of the five mice; all five were euthanized on day 42 due to progressive weight loss although none had evidence of tumor progression.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 521064-34-6
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Appearance Solid
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Molecular Weight 390.66
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Formula C16H13BrClN5
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Color Off-white to light yellow
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SMILES
ClC1=CC(C2=NC(NC3=CC=C(C=C3)Br)=NC(N)=N2)=C(C)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 5 mg/mL (12.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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 Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[2]. Gong B, et al. Synthesis, SAR, and antitumor properties of diamino-C,N-diarylpyrimidine positional isomers: inhibitors of lysophosphatidic acid acyltransferase-beta. Bioorg Med Chem Lett. 2004 May 3;14(9):2303-8. [Content Brief]
[3]. Hideshima T, et al. Antitumor activity of lysophosphatidic acid acyltransferase-beta inhibitors, a novel class of agents, in multiple myeloma. Cancer Res. 2003 Dec 1;63(23):8428-36. [Content Brief]
[4]. Pagel JM, et al. Induction of apoptosis using inhibitors of lysophosphatidic acid acyltransferase-beta and anti-CD20 monoclonal antibodies for treatment of human non-Hodgkin's lymphomas. Clin Cancer Res. 2005 Jul 1;11(13):4857-66. [Content Brief]
[5]. Douvas MG, et al. Effect of lysophosphatidic acid acyltransferase-beta inhibition in acute leukemia. Leuk Res. 2006 Aug;30(8):1027-36. [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. 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 | 2.5598 mL | 12.7989 mL | 25.5977 mL | 63.9943 mL |
| 5 mM | 0.5120 mL | 2.5598 mL | 5.1195 mL | 12.7989 mL | |
| 10 mM | 0.2560 mL | 1.2799 mL | 2.5598 mL | 6.3994 mL |
CT 32228 Related Classifications
HY-178712 Related Classifications
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