| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
| Other Sizes |
| Targets |
IC50: 15 nM (DGKα)[1]
Diacylglycerol kinase alpha (DGKα). BMS-684 is a highly selective small-molecule inhibitor of DGKα with an IC50 of 15 nM. It demonstrates over 100-fold selectivity against other type I DGK isoforms such as DGKβ and DGKγ. DGKα is a lipid kinase that phosphorylates diacylglycerol (DAG) to phosphatidic acid (PA), regulating DAG-mediated signaling pathways involved in T cell activation and immune regulation. |
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| ln Vitro |
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. It inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. The compound activates T cells and has potential antitumor activity. Its immunostimulatory activity is enhanced compared to less selective inhibitors.
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| ln Vivo |
In vivo, BMS-684 has potential for preventing and treating immune-related diseases by activating T cells. Its potent and isoform-specific inhibition supports mechanistic studies and therapeutic exploration targeting DGKα. The compound is being investigated for cancer and immune regulation applications.
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| Enzyme Assay |
In vitro enzyme activity assays for BMS-684 involve measuring its ability to inhibit DGKα kinase activity. Recombinant DGKα enzyme is incubated with diacylglycerol substrate in the presence of ATP and increasing concentrations of the compound. Kinase activity is measured by detecting the production of phosphatidic acid, and the IC50 is determined from dose-response curves (IC50 = 15 nM).
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| Cell Assay |
In vitro cellular assays for BMS-684 involve treating T cells with the compound and measuring its effects on T cell activation. Readouts include T cell proliferation, cytokine production, and activation marker expression. The compound's ability to activate T cells confirms its DGKα inhibitory activity in a cellular context.
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| Animal Protocol |
In vivo efficacy of BMS-684 would be evaluated in animal models of cancer and immune-related diseases. The compound could be administered via injection. Efficacy endpoints would include tumor growth inhibition, T cell activation, and immune response modulation. Specific in vivo data is limited in the available literature.
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| ADME/Pharmacokinetics |
BMS-684 has a molecular weight of 454.52 g/mol and a molecular formula of C27H26N4O3. Its IUPAC name is 4-(4-benzhydrylpiperazin-1-yl)-1-methyl-3-nitroquinolin-2-one. The compound has a purity of ≥95%. It is structurally related to the dual DGKα/ζ inhibitor BMS-502.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for BMS-684 in the provided literature. As a research compound, its safety profile would be an important consideration for in vivo applications. Potential toxicities could be related to its immunomodulatory effects. Standard preclinical safety studies would be required.
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| References | |
| Additional Infomation |
BMS-684 is a highly selective DGKα inhibitor with an IC50 of 15 nM. It shows over 100-fold selectivity against other type I DGK isoforms. BMS-684 activates T cells and has potential for cancer and immune-related disease research. It has a molecular formula of C27H26N4O3 and a molecular weight of 454.52. It is a research tool and is not approved for clinical use.
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| CAS # |
313552-29-3
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| Appearance |
Light yellow to yellow solid powder
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| SMILES |
CN(C1=CC=CC=C1C(N2CCN(C(C3=CC=CC=C3)C4=CC=CC=C4)CC2)=C5[N+]([O-])=O)C5=O
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~14.3 mg/mL (~31.4 mM; with ultrasonication and warming)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.43 mg/mL (3.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (14.3 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.43 mg/mL (3.15 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (14.3 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 1.43 mg/mL (3.15 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (14.3 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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