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BI-D1870 - ≥98%, high purity , CAS No.501437-28-1, Inhibitor of ribosomal protein S6 kinase A1;Inhibitor of ribosomal protein S6 kinase A2;Inhibitor of ribosomal protein S6 kinase A3;Inhibitor of ribosomal protein S6 kinase A6

  • Moligand™
  • ≥98%
Item Number
B126041
Grouped product items
SKUSizeAvailabilityPrice Qty
B126041-10mg
10mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$260.90
B126041-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$587.90
B126041-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$593.90
B126041-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$1,069.90

Basic Description

SynonymsBI-D1870|501437-28-1|2-((3,5-difluoro-4-hydroxyphenyl)amino)-8-isopentyl-5,7-dimethyl-7,8-dihydropteridin-6(5H)-one|BI-D 1870|2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one|2-[(3,5-DIFLUORO-4-HYDROXYPHENYL)AMINO]-7,8-DI
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsBI-D1870 is a cell permeable, ATP-competitive inhibitor of the four isoforms of ribosomal S6 kinase (p90 RSK) (IC50's at 100μM ATP: RSK1 = 31nM, RSK2 = 24nM, RSK3 = 18nM, RSK4 = 15nM). It does not significantly inhibit 10 other AGC kinases, and over 40 ot
Storage TempProtected from light,Store at -20°C,Argon charged
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of ribosomal protein S6 kinase A1;Inhibitor of ribosomal protein S6 kinase A2;Inhibitor of ribosomal protein S6 kinase A3;Inhibitor of ribosomal protein S6 kinase A6
Product Description

BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 of 31 nM/24 nM/18 nM/15 nM, respectively; 10- to 100-fold selectivity for RSK than MST2, GSK-3β, MARK3, CK1 and Aurora B
A cell permeable, ATP-competitive inhibitor.

Associated Targets

PPBP Tbio Platelet basic protein 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

DYRK1A Tchem Dual specificity tyrosine-phosphorylation-regulated kinase 1A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PAK5 Tchem Serine/threonine-protein kinase PAK 5 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

SRC Tclin Proto-oncogene tyrosine-protein kinase Src 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ROCK2 Tclin Rho-associated protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

STK3 Tchem Serine/threonine-protein kinase 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HIPK3 Tchem Homeodomain-interacting protein kinase 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

IKBKB Tchem Inhibitor of nuclear factor kappa-B kinase subunit beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HIPK2 Tchem Homeodomain-interacting protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM1 Tchem Serine/threonine-protein kinase pim-1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM2 Tchem Serine/threonine-protein kinase pim-2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PLK1 Tchem Serine/threonine-protein kinase PLK1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PIM3 Tchem Serine/threonine-protein kinase pim-3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PKN2 Tchem Serine/threonine-protein kinase N2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MKNK2 Tchem MAP kinase-interacting serine/threonine-protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA2 Tchem Ribosomal protein S6 kinase alpha-2 4 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA6 Tchem Ribosomal protein S6 kinase alpha-6 4 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK12 Tchem Mitogen-activated protein kinase 12 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK8 Tchem Mitogen-activated protein kinase 8 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MKNK1 Tchem MAP kinase-interacting serine/threonine-protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKD1 Tchem Serine/threonine-protein kinase D1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

LCK Tclin Tyrosine-protein kinase Lck 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPKAPK3 Tchem MAP kinase-activated protein kinase 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKB Tchem Aurora kinase B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKC Tchem Aurora kinase C 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK1 Tchem Serine/threonine-protein kinase Chk1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CHEK2 Tchem Serine/threonine-protein kinase Chk2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EEF2K Tchem Eukaryotic elongation factor 2 kinase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PAK4 Tchem Serine/threonine-protein kinase PAK 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PAK6 Tchem Serine/threonine-protein kinase PAK 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

JAK2 Tclin Tyrosine-protein kinase JAK2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKACA Tchem cAMP-dependent protein kinase catalytic subunit alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK13 Tchem Mitogen-activated protein kinase 13 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK14 Tchem Mitogen-activated protein kinase 14 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA3 Tchem Ribosomal protein S6 kinase alpha-3 5 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PDPK1 Tchem 3-phosphoinositide-dependent protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one
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
Canonical SMILES CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
Isomeric SMILES CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C
PubChem CID 25023738
Molecular Weight 391.42

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
C2321417Certificate of AnalysisFeb 13, 2023 B126041
C2321424Certificate of AnalysisFeb 13, 2023 B126041
C2321485Certificate of AnalysisFeb 13, 2023 B126041
C2321490Certificate of AnalysisFeb 13, 2023 B126041

Chemical and Physical Properties

SolubilityDMSO 78 mg/mL Water <1 mg/mL Ethanol <1 mg/mL;≥ 19.55mg/mL in DMSO
Sensitivitylight sensitive

Related Documents

References

1. Sapkota GP, Cummings L, Newell FS, Armstrong C, Bain J, Frodin M, Grauert M, Hoffmann M, Schnapp G, Steegmaier M et al..  (2007)  BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo..  Biochem J,  401  (1): (29-38).  [PMID:17040210]

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