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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | (2S)-2-[[9-isopropyl-6-[[4-(2-pyridyl)phenyl]methylamino]purin-2-yl]amino]butan-1-ol | (S)-CR8 | CR8, (S)-Isomer | (2S)-2-{[9-(propan-2-yl)-6-{[4-(pyridin-2-yl)benzyl]amino}-9H-purin-2-yl]amino}butan-1-ol | GTPL11064 | Q27167221 | (S)-2-((9-Isopropyl-6-(( |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent, 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 Temp | Protected from light,Store at -20°C,Desiccated |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5;Inhibitor of dual specificity tyrosine phosphorylation regulated kinase 1A |
Note | Wherever 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)。
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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | (2S)-2-[[9-propan-2-yl-6-[(4-pyridin-2-ylphenyl)methylamino]purin-2-yl]amino]butan-1-ol |
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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 |
PubChem CID | 25211051 |
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CAS Registry No. | 1084893-56-0 |
ChEMBL Ligand | CHEMBL1615221 |
RCSB PDB Ligand | SLQ |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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I2403314 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403315 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403319 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403320 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403321 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403327 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403329 | Certificate of Analysis | May 31, 2024 | C275643 |
I2403331 | Certificate of Analysis | May 31, 2024 | C275643 |
Solubility | Soluble in ethanol to 25 mM and in DMSO to 10 mM |
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Sensitivity | air and light sensitive |
Starting at $142.90
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] [10.1021/op500134e] |
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, 2 (4): (230-246). [PMID:32259059] |