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(R)-CR8 , CAS No.294646-77-8, Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 5

Moligand™

CAS#: 294646-77-8
Formula: C₂₄H₂₉N₇O
Molecular Weight: 431.53
PubChem CID: 10224714

Item Number

R613113

Grouped product items
SKU	Size	Availability	Price
R613113-1mg	1mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$57.90
R613113-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$171.90
R613113-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$256.90
R613113-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$544.90
R613113-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$870.90
R613113-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,399.90

View related series

Apoptosis CDK Cell Cycle/DNA Damage cyclin dependent kinase 1 Inhibitor cyclin dependent kinase 5 Inhibitor Molecular Glues PROTAC

Basic Description

Synonyms	294646-77-8\|CR8, (R)-Isomer\|(R)-CR8\|(2R)-2-({9-(1-methylethyl)-6-[(4-pyridin-2-ylbenzyl)amino]-9H-purin-2-yl}amino)butan-1-ol\|(R)?-?CR8\|1-Butanol, 2-[[9-(1-methylethyl)-6-[[[4-(2-pyridinyl)phenyl]methyl]amino]-9H-purin-2-yl]amino]-, (2R)-\|(R)-2-((9-Isopro
Specifications & Purity	Moligand™
Biochemical and Physiological Mechanisms	CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). CR8 is a more potent pyridyl analogue of roscovitine (Cat. No. R7772). In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in
Storage Temp	Store at -20°C
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
Product Description	（R）-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.

Associated Targets

CDK1 Tchem Cyclin-dependent kinase 1 0 Activities

Discover Target: CDK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCNE1 Tchem G1/S-specific cyclin-E1 0 Activities

Discover Target: CCNE1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCNH Tbio Cyclin-H 0 Activities

Discover Target: CCNH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK4 Tclin Cyclin-dependent kinase 4 0 Activities

Discover Target: CDK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CCNT1 Tchem Cyclin-T1 0 Activities

Discover Target: CCNT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK5R1 Tchem Cyclin-dependent kinase 5 activator 1 0 Activities

Discover Target: CDK5R1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK5 Tchem Cyclin-dependent-like kinase 5 0 Activities

Discover Target: CDK5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3A Tclin Glycogen synthase kinase-3 alpha 0 Activities

Discover Target: GSK3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSNK1A1 Tchem Casein kinase I isoform alpha 0 Activities

Discover Target: CSNK1A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	(2R)-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-/m1/s1
InChi Key	HOCBJBNQIQQQGT-LJQANCHMSA-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	10224714
Molecular Weight	431.53

PubChem CID

CAS Registry No.

BindingDB Ligand

ChEMBL Ligand

DrugBank Ligand

RCSB PDB Ligand

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H302:Harmful if swallowed
Precautionary Statements	P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help.

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. Słabicki M, Kozicka Z, Petzold G, Li YD, Manojkumar M, Bunker RD, Donovan KA, Sievers QL, Koeppel J, Suchyta D et al.. (2020) The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.. Nature, 585 (7824): (293-297). [PMID:32494016]

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