59259-77-7
Chemical Structure
8-Br-ADPR
Synonym(s): 8-Bromoadenosine-5'-O-diphosphoribose
- CAS No.: 59259-77-7
- Formula:C15H22BrN5O14P2
- Molecular Weight:638.21
InChIKey: DPZGAPGUTMHLAW-DBINCYRJSA-N
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
Biological Activity: 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[1][2].
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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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References
- [1]. Rah SY, et al. CD38/ADP-ribose/TRPM2-mediated nuclear Ca2+ signaling is essential for hepatic gluconeogenesis in fasting and diabetes. Exp Mol Med. 2023;55(7):1492-1505. [Content Brief]
- [2]. Rah S Y, et al. ADP-ribose/TRPM2-mediated Ca2+ signaling is essential for cytolytic degranulation and antitumor activity of natural killer cells[J]. Scientific reports, 2015, 5(1): 9482.
