8-Br-ADPR
Based on 1 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 59259-77-7
- Formule: C15H22BrN5O14P2
- Masse moléculaire:638.21
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) 8-Br-ADPR
More
Activité biologique
|
CaMK II |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
300 μM
Compound: 4, 8-Br-ADPR
|
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
|
[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.
-
Cell Line:Murine natural killer (NK) cells
-
Concentration:100 μM
-
Incubation Time:20 min (preincubation)
-
Result:Blocked the B16F10-induced translocation of perforin and granzyme B towards the immunological synapse between NK cells and B16F10 cells.
-
Cell Line:Murine natural killer (NK) cells
-
Concentration:100 μM
-
Incubation Time:20 min (preincubation)
-
Result:Inhibited the PME-induced translocation of perforin and granzyme B from intracellular granules to plasma membrane-enriched fractions.
-
Cell Line:Murine natural killer (NK) cells
-
Concentration:100 μM
-
Incubation Time:20 min (preincubation)
-
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.
-
Animal Model:C57BL/6J mice with Physiological fasting (male, 8-12 weeks old)[1]
-
Dosage:32 mg/kg
-
Administration:i.v.; single dose
-
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.
-
Animal Model:B6.BKS(D)-Leprdb/J mice with Diabetes (db/db) (male, 8-12 weeks old)[1]
-
Dosage:32 mg/kg
-
Administration:i.v.; single dose
-
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
-
CAS No. 59259-77-7
-
Masse moléculaire 638.21
-
Formule C15H22BrN5O14P2
-
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
-
Synonyms
8-Bromoadenosine-5'-O-diphosphoribose
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
8-Br-ADPR Related Classifications
HY-134261 Related Classifications
Powered by Bioz