872573-93-8
872573-93-8 structure
- Name: RO-3306
- Chemical Name: Ro-3306
- CAS Number: 872573-93-8
- Molecular Formula: C18H13N3OS2
- Molecular Weight: 351.445
- Catalog: Biochemical Inhibitor Cell Cycle CDK inhibitor
- Create Date: 2017-05-16 00:57:58
- Modify Date: 2024-01-06 18:18:09
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Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
| Name | Ro-3306 |
|---|---|
| Synonyms |
4(5H)-Thiazolone, 5-(6-quinolinylmethylene)-2-[(2-thienylmethyl)amino]-, (5Z)-
(5Z)-5-(quinolin-6-ylmethylidene)-2-[(thiophen-2-ylmethyl)amino]-1,3-thiazol-4(5H)-one (5Z)-5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethylamino)-1,3-thiazol-4-one (5Z)-5-(6-Quinolinylmethylene)-2-[(2-thienylmethyl)amino]-1,3-thiazol-4(5H)-one |
| Description | Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively. |
|---|---|
| Related Catalog | |
| Target |
CDK1:20 nM (Ki) CDK1/cyclinB1:35 nM (Ki) CDK1/cyclin A:110 nM (Ki) CDK2/cyclinE:340 nM (Ki) PKCδ:318 nM (Ki) SGK:497 nM (Ki) ERK:1980 nM (Ki) |
| In Vitro | RO-3306 is an ATP-competitive inhibitor, and inhibits CDK1/cyclin A complexes with Ki of 110 nM. RO-3306 blocks the cell cycle in the G2/M phase of human cancer cells. RO-3306 (4 μM) induces apoptosis in cancer cells[1]. RO-3306 (5 μM) induces G2/M-phase cell cycle arrest and apoptosis of AML cells in a time-dependent manner. RO-3306 treatment significantly increases the percentage of Annexin V-positive cells in G1-phase cells without affecting the cell cycle distribution. RO-3306 enhances p53-mediated apoptosis. RO-3306 cooperates with Nutlin-3 in activating Bax and inducing mitochondrial apoptosis. RO-3306 (5 μM) downregulates antiapoptotic p21, Bcl-2 and survivin protein expression in AML. RO-3306 inhibits p53-induced p21 synthesis. RO-3306 does not inhibit RNA polymerase II CTD phosphorylation[2]. RO-3306 (10 μM) effectively arrests oocyte maturation. RO-3306 reduces the blastocyst formation in oocytes[3]. |
| Kinase Assay | The CDK assays are run by using recombinant human CDK/cyclin complexes (CDK1/cyclin B1, CDK1/cyclin A, CDK2/cyclin E, and CDK4/cyclin D) expressed and isolated from Hi5 insect cells. GST-cyclin B1, CDK1, GST-cyclin-E, CDK2, GST-CDK4, and cyclin D, are used in the assay. The GST-tagged proteins are coexpressed and purified in complex with their partners. All assays use a His-6-tagged fragment of pRB (amino acids 385-928) as a substrate. The protein is expressed from a construct. It is expressed in M15 Escherichia coli cells and bound on a Ni-chalated agarose column pretreated with 1 mM imidazole and eluted with 500 mM imidazole. The eluted protein is dialyzed against 20 mM Hepes, pH 7/6.25 mM MgCl2/1.5 mM DTT, aliquoted, and stored at −80°C. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 569.1±60.0 °C at 760 mmHg |
| Molecular Formula | C18H13N3OS2 |
| Molecular Weight | 351.445 |
| Flash Point | 298.0±32.9 °C |
| Exact Mass | 351.049988 |
| PSA | 111.38000 |
| LogP | 3.24 |
| Appearance | white to light brown |
| Vapour Pressure | 0.0±1.6 mmHg at 25°C |
| Index of Refraction | 1.746 |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: soluble5mg/mL, clear |
| RIDADR | NONH for all modes of transport |
|---|