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Ro-3306

Catalog No. T2356 CAS 872573-93-8

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is <15-fold higher than a diverse panel of human kinases.

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Ro-3306, CAS 872573-93-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 32.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 93.00
25 mg	In stock	$ 158.00
50 mg	In stock	$ 228.00
100 mg	In stock	$ 372.00
200 mg	In stock	$ 549.00
500 mg	In stock	$ 869.00
1 mL * 10 mM (in DMSO)	In stock	$ 75.00

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Purity: 99.74%

Purity: 98.59%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.
Targets&IC50	CDK1:20 nM(Ki), PKCδ:318 nM(Ki), ERK:1980 nM(Ki), SGK:497 nM(Ki)
In vivo	In HCT116, SW480, and HeLa cell lines, treatment with RO-3306 for 20 hours resulted in a complete cell cycle arrest at the G2/M phase. RO-3306 (10 μM) effectively inhibits oocyte maturation. The compound demonstrates inhibition of CDK1/cyclin B1 (Ki: 35 nM), CDK1/cyclin A (Ki: 110 nM), CDK2/cyclin E (Ki: 340 nM), and CDK4/cyclin D (Ki>2000 nM) activities. Additionally, RO-3306 significantly impedes the proliferation of HCT116 and SW480 cells. Compared to non-tumorigenic cells (MCF 10A and MCF 12A), RO-3306 exhibits a stronger pro-apoptotic effect on cancerous cells (HCT116 and SW480).
Kinase Assay	CDK assay: The activity of CDK1 cyclin B1, CDK1 cyclin A, CDK2 cyclin E, and CDK4 cyclin D is measured by a homogeneous time-resolved fluorescence assay in a 96-well format. The assay buffer contained 25 mM Hepes, 6.25 mM MgCl2, 0.003% Tween 20, 0.3 mg/mL BSA, 1.5 mM DTT, and ATP as follows: 162 μM (CDK1), 90 mM (CDK2), or 135 μM (CDK4). CDK1 and CDK2 buffer contained 10 mM MgCl2. Test compounds are diluted in assay buffer to 3-fold their final concentration in 20 μL, and the reaction is started by the addition of a 40 μL assay buffer containing the pRB substrate (0.185 μM). The plates are incubated at 37°C for 30 min with constant agitation, and the reaction is terminated by the addition of 15 μL of 1.6 μM anti-phospho pRB antibody (Ser-780) in 25 mM Hepes, 24 mM EDTA, and 0.2 mg/mL BSA. After an additional 30 min of incubation with shaking, 15μL of 3 nM Lance-Eu-W1024-labeledanti-rabbitIgG and 60 nM Alophycocyanin-conjugated anti-His-6 antibody in 25 mM Hepes, and 0.5 mg/mL BSA is added and incubated for 1 h. The plates are read in the Victor-V multi- label reader at excitation 340 nm and emission 615 nm and 665 nm. The IC50 values are calculated from the readings at 665 nm and normalized for Europium readings at 615 nm. Ki values are calculated according to the equation: Ki= IC50/(1 + S/Km ), where S is the ATP concentration in the assay and Km is the Michaelis-Menten constant for ATP. The inhibitory activity against the panel of kinases is determined by the IMAP assay technology.
Cell Research	Log phases cells (25,000) are seeed in 96-well plates and incubated in a 37℃ incubator with CO2, After 24 h, different concentrations of RO-3306 are administered to determine the drug concentrations required to achieve a 50% growth inhibition (IC50). MTT (20 μL, 5 mg/mL stock solution in saline) is added to each well and the cells are incubated for 4 h. Supernatants are removed and formazan crystals from viable cells are solubilized with 200 μL anhydrous DMSO. The absorbance is detected with a 550 model microplate reader at the 565 nm wavelength.(Only for Reference)

Molecular Weight	351.45
Formula	C18H13N3OS2
CAS No.	872573-93-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 12.5 mg/mL (35.57 mM)

References and Literature

1. Vassilev LT, et al. Proc Natl Acad Sci U S A. 2006, 103(28), 10660-10665. 2. Jang WI, et al. Anim Reprod Sci. 2014, 144(3-4), 102-108. 3. Xia Q, et al. Int J Oncol. 2014, 44(3), 735-744. 4. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity[J]. Biochemical and biophysical research communications. 2019 Jun 11;513(4):967-973.

Citations

1. Zhang Y, Hong X, Hua S, et al. Reconstitution and mechanistic dissection of the human microtubule branching machinery. Journal of Cell Biology. 2022, 221(7): e202109053 2. Chen C, Zhang X, Wang Y, et al. Translational and Post-translational Control of Human Naïve versus Primed Pluripotency. iScience. 2021: 103645. 3. Ou J, Li H, Qiu P, et al. CDK9 modulates circadian clock by attenuating REV-ERBα activity. Biochemical and Biophysical Research Communications. 2019 Jun 11;513(4):967-973 4. Guo S, Lei X, Chang Y, et al.SARS-CoV-2 hijacks cellular kinase CDK2 to promote viral RNA synthesis.Signal Transduction and Targeted Therapy.2022, 7(1): 1-12. 5. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library TGF-beta/Smad Compound Library Tyrosine Kinase Inhibitor Library Bioactive Compounds Library Max Metabolism Compound Library Anti-Metabolism Disease Compound Library Reprogramming Compound Library Cell Cycle Compound Library Anti-Obesity Compound Library

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Keywords

Ro-3306 872573-93-8 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling MAPK Metabolism Tyrosine Kinase/Adaptors ERK CDK PKC SGK PKA Cyclin dependent kinase Ro3306 Inhibitor Ro 3306 inhibit inhibitor

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