8-Br-ADPR
8-Br-ADPR (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR is widely used in studies related to diseases such as diabetes, melanoma and lymphoma.
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- CAS No.: 59259-77-7
- Formula: C15H22BrN5O14P2
- Molecular Weight:638.21
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CaMK II |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
300 μM
Compound: 4, 8-Br-ADPR
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Antagonist activity at human TRPM2 expressed in HEK293 cells assessed as inhibition of ADPR-induced maximum outward potassium current at +15 mV by whole-cell patch-clamp electrophysiology
Antagonist activity at human TRPM2 expressed in HEK293 cells assessed as inhibition of ADPR-induced maximum outward potassium current at +15 mV by whole-cell patch-clamp electrophysiology
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[PMID: 24304219] |
8-Br-ADPR (100 μM; preincubated prior to glucagon treatment) specifically blocks glucagon-induced sustained nuclear calcium signals in mouse primary hepatocytes, without altering cytosolic calcium signals[1].
8-Br-ADPR (100 μM; 30 min preincubated before ADPR treatment) completely blocks ADPR-induced calcium flux between the perinuclear space and nucleoplasm in isolated nuclei from mouse primary hepatocytes[1].
8-Br-ADPR (100 μM; 30 min preincubated before 100 nM glucagon treatment for 4 h) significantly reduces glucagon-induced G6pc and Pck1 mRNA expression in mouse primary hepatocytes[1].
8-Br-ADPR (100 μM; 20 min) inhibits B16F10-induced translocation of perforin and granzyme B to the immunological synapse in murine NK cells[2].
8-Br-ADPR (100 μM; 20 min) reduces the cytolytic activity of murine NK cells against B16F10 melanoma target cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine natural killer (NK) cells
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Concentration:100 μM
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Incubation Time:20 min (preincubation)
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Result:Blocked the B16F10-induced translocation of perforin and granzyme B towards the immunological synapse between NK cells and B16F10 cells.
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Cell Line:Murine natural killer (NK) cells
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Concentration:100 μM
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Incubation Time:20 min (preincubation)
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Result:Inhibited the PME-induced translocation of perforin and granzyme B from intracellular granules to plasma membrane-enriched fractions.
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Cell Line:Murine natural killer (NK) cells
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Concentration:100 μM
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Incubation Time:20 min (preincubation)
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Result:Inhibited B16F10-induced granzyme B secretion from NK cells, reducing the amount of granzyme B released into the culture medium.
8-Br-ADPR (32 mg/kg; i.v.; single dose) reduces pyruvate-induced blood glucose levels in diabetic db/db mice by inhibiting hepatic gluconeogenic gene expression and CRE-mediated transcriptional activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice with Physiological fasting (male, 8-12 weeks old)[1]
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Dosage:32 mg/kg
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Administration:i.v.; single dose
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Result:Reduced hepatic CRE luciferase activity.
Lowered liver G6pc and Pck1 mRNA levels by ~50% each.
Decreased pyruvate tolerance test blood glucose levels by ~30-40% across 0-90 minutes post-pyruvate injection.
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Animal Model:B6.BKS(D)-Leprdb/J mice with Diabetes (db/db) (male, 8-12 weeks old)[1]
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Dosage:32 mg/kg
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Administration:i.v.; single dose
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Result:Reduced hepatic CRE luciferase activity.
Decreased liver G6pc mRNA levels by ~40% and Pck1 mRNA levels by ~30%.
Reduced pyruvate tolerance test blood glucose levels by ~60-70% across all time points.
Chemical Information
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CAS No. 59259-77-7
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Molecular Weight 638.21
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Formula C15H22BrN5O14P2
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C(Br)=NC3=C2N=CN=C3N)O[C@@H]1COP(OP(OC[C@H]4OC(O)[C@H](O)[C@@H]4O)(O)=O)(O)=O
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Synonyms
8-Bromoadenosine-5'-O-diphosphoribose
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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