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(S)-CR8 - ≥98%, high purity , CAS No.1084893-56-0, Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A

  • Moligand™
  • ≥98%
Item Number
C275643
Grouped product items
SKUSizeAvailabilityPrice Qty
C275643-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$139.90
C275643-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$469.90
C275643-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$749.90
C275643-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,499.90

Potent, selective, cell-permeable cyclin-dependent kinase (CDK) 1, 2, 5, 7 and 9 inhibitor

Basic Description

SynonymsCR8, (S)-Isomer|1084893-56-0|(S)-CR8|(2S)-2-[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol|(2S)-2-[[9-propan-2-yl-6-[[4-(2-pyridinyl)phenyl]methylamino]-2-purinyl]amino]-1-butanol|CHEMBL1615221|(2s)-2-({9-(1-Methylethyl)-
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsPotent, selective, cell-permeable cyclin-dependent kinase (CDK) 1, 2, 5, 7 and 9 inhibitor (IC 50 = 41 - 400 nM). (R)-DRF053 analog. More potent than roscovirtine. Apoptosis inducer. GSK-3α/β (glycogen synthase kinase-3α/β) inhibitor.
Storage TempProtected from light,Store at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM)。

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 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)

CDK9 Tchem Cyclin-dependent kinase 9 0 Activities

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

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

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

Names and Identifiers

IUPAC Name (2S)-2-[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol
INCHI InChI=1S/C24H29N7O/c1-4-19(14-32)28-24-29-22(21-23(30-24)31(15-27-21)16(2)3)26-13-17-8-10-18(11-9-17)20-7-5-6-12-25-20/h5-12,15-16,19,32H,4,13-14H2,1-3H3,(H2,26,28,29,30)/t19-/m0/s1
InChi Key HOCBJBNQIQQQGT-IBGZPJMESA-N
Canonical SMILES CCC(CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=C(C=C3)C4=CC=CC=N4
Isomeric SMILES CC[C@@H](CO)NC1=NC(=C2C(=N1)N(C=N2)C(C)C)NCC3=CC=C(C=C3)C4=CC=CC=N4
PubChem CID 25211051
Molecular Weight 431.53

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySoluble in ethanol to 25 mM and in DMSO to 10 mM
Sensitivityair and light sensitive

Related Documents

References

1. Bettayeb K, Oumata N, Echalier A, Ferandin Y, Endicott JA, Galons H, Meijer L.  (2008)  CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases..  Oncogene,  27  (44): (5797-807).  [PMID:18574471]
2. Toth K et al..  (2019)  Encoding the ß-Arrestin Trafficking Fate of Ghrelin Receptor GHSR1a: C-Tail-Independent Molecular Determinants in GPCRs..  ACS Pharmacol Transl Sci,  (4): (230-246).  [PMID:32259059]

Solution Calculators