217699
RO-3306
≥95% (HPLC), solid, Cdk1 inhibitor, Calbiochem®
Synonym(s):
Cdk1 Inhibitor IV, RO-3306
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About This Item
Empirical Formula (Hill Notation):
C18H13N3OS2
Molecular Weight:
351.45
UNSPSC Code:
12352200
NACRES:
NA.77
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product name
Cdk1 Inhibitor IV, RO-3306, RO-3306 is a cell-permeable, potent and ATP-competitive inhibitor of Cdk1 (Ki = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively).
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
brown
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
A cell-permeable quinolinyl thiazolinone compound that acts as a potent and ATP-competitive inhibitor of Cdk1 (Ki = 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively). It affects Cdk2/E, PKCδ, and SGK only at much higher concentrations (Ki = 340, 318, and 497 nM, respectively), and shows little effect against Cdk4/D and six other commonly studied kinases (Ki ≥ 2 µM). Short-term treatment for up to 20 hrs results in fully reversible G2/M cell cycle arrest, while prolonged treament (>48 hrs) results in apoptotic cell death in proliferating cancer cells, but not in nontumorigenic epithelial cell lines. Also available as a 10 mM solution in DMSO (Cat. No. 217721).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk1
Cdk1
Product competes with ATP.
Reversible: no
Target Ki: 35 nM and 110 nM for Cdk1/B1 and Cdk1/A, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Vassilev, L.T., et al. 2006. Proc. Natl. Acad. Sci. USA103, 10660.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Yuji Nakayama et al.
Journal of cellular biochemistry, 115(4), 763-771 (2014-01-24)
Genistein, an isoflavone abundantly present in soybeans, possesses anticancer properties and induces growth inhibition including cell cycle arrest and apoptosis. Although abnormal cell division, such as defects in chromosome segregation and spindle formation, and polyploidization have been described, the mechanisms
Pia-Amata Leimbacher et al.
Molecular cell, 74(3), 571-583 (2019-03-23)
In mitosis, cells inactivate DNA double-strand break (DSB) repair pathways to preserve genome stability. However, some early signaling events still occur, such as recruitment of the scaffold protein MDC1 to phosphorylated histone H2AX at DSBs. Yet, it remains unclear whether
Beate Vajen et al.
International journal of molecular sciences, 23(9) (2022-05-15)
Chromosomal instability (CIN) can be a driver of tumorigenesis but is also a promising therapeutic target for cancer associated with poor prognosis such as triple negative breast cancer (TNBC). The treatment of TNBC cells with defects in DNA repair genes
Ryan P Barnes et al.
Nature structural & molecular biology, 29(7), 639-652 (2022-07-01)
Oxidative stress is a primary cause of cellular senescence and contributes to the etiology of numerous human diseases. Oxidative damage to telomeric DNA has been proposed to cause premature senescence by accelerating telomere shortening. Here, we tested this model directly
Olivier Brison et al.
Nature structural & molecular biology, 30(4), 539-550 (2023-04-07)
Genome integrity requires replication to be completed before chromosome segregation. The DNA-replication checkpoint (DRC) contributes to this coordination by inhibiting CDK1, which delays mitotic onset. Under-replication of common fragile sites (CFSs), however, escapes surveillance, resulting in mitotic chromosome breaks. Here
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