BI-D1870 | 1924

Cell-permeable. ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK) (IC₅₀'s at 100 µM ATP: RSK1 = 31 nM, RSK2 = 24 nM, RSK3 = 18 nM, RSK4 = 15 nM). Does not significantly inhibit 10 other AGC kinases, and over 40 other protein kinases at 100X concentrations. In addition, BI-D1870 completely prevents PMA-induced TSC2 (a regulator of mTORC1) phosphorylation at Ser¹⁷⁹⁸.

BI-D1870 is an ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK) (IC₅₀'s at 100 µM ATP: RSK1 = 31 nM, RSK2 = 24 nM, RSK3 = 18 nM, RSK4 = 15 nM). Does not significantly inhibit 10 other AGC kinases, and over 40 other protein kinases at 100X concentrations. In addition, BI-D1870 completely prevents PMA-induced TSC2 (a regulator of mTORC1) phosphorylation at Ser¹⁷⁹⁸.

1924 | BI-D1870 DataSheet

Alternate Name/Synonyms: 2-[(3,5-Difluoro-4-hydroxyphenyl)amino]-7,8-dihydro-5,7-dimethyl-8-(3-methylbutyl)-6(5H)-pteridone

Appearance: Pale orange solid

Formulation: N/A

CAS Number: 501437-28-1

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₁₉H₂₃F₂N₅O₂

Molecular Weight: 391.42

Cell-Permeable?: Yes

Purity: ≥98% by TLC

Solubilities: DMSO (>25 mg/ml)

Handling: Protect from light and air

Country of Origin: USA

Tag Line: An ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK)

MDL Number: MFCD11223662

PubChem CID: 25023738

SMILES: CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C

InChi: InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17 (15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)

InChi Key: DTEKTGDVSARYDS-UHFFFAOYSA-N