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CX-5461

Catalog No. T2100 CAS 1138549-36-6

CX-5461, a selective inhibitor of rRNA synthesis, suppresses Pol I-driven transcription of rRNA.

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CX-5461, CAS 1138549-36-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 35.00
2 mg	In stock	$ 47.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 163.00
25 mg	In stock	$ 291.00
50 mg	In stock	$ 492.00
100 mg	In stock	$ 717.00
500 mg	In stock	$ 1,470.00

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Purity: 99.25%

Purity: 98.01%

Purity: 95.44%

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Description	CX-5461, a selective inhibitor of rRNA synthesis, suppresses Pol I-driven transcription of rRNA.
Targets&IC50	Pol I-driven transcription of rRNA:142 nM
In vitro	CX-5461 demonstrates the capacity to inhibit cell proliferation in various cell lines, notably HCT-116 (EC50=167 nM), A375 (EC50=58 nM), and MIA PaCa-2 (EC50=74 nM). In solid tumor cells, CX-5461 induces autophagy or senescence rather than apoptosis. For instance, in melanoma A375 cells and pancreatic cancer MIA PaCa-2 cells, its effects are quantified with Pol I IC50 values of 113 nM and 54 nM, respectively, while showing significantly less effect on Pol II (Pol II IC50 > 25 μM for A375 and ~25 mM for MIA PaCa-2). Furthermore, in HCT-116 cells, CX-5461 selectively inhibits rRNA synthesis, with an observed Pol I IC50 of 142 nM and minimal impact on Pol II (IC50 > 25 μM).
In vivo	In a mouse model of xenograft human solid tumors, oral administration of CX-5461 (50 mg/kg) demonstrated antitumor activity against solid tumors.
Kinase Assay	Pol I and Pol II Transcription Assay: Two short-lived RNA transcripts (half-lives ~20-30 minutes), one produced by Pol I and another by Pol II, are quantitated by qRT-PCR as a measure of CX-5461-related effects on transcription. The 45S pre-rRNA served as the Pol I transcript and the mRNA for the protooncogene c-myc served as the comparator Pol II transcript. Both Pol I and Pol II transcription are known to be affected by general cellular stress. To minimize the potential effects of such stress, cells are exposed to test agents for only a short period of time (2 hours). This is sufficient time for these transcripts to be reduced by greater than 90% if CX-5461 affects their synthesis.
Cell Research	Cells are plated on 96-well plates and treated the next day with dose response of CX-5461 for 96 hours. Cell viability is determined using Alamar Blue and CyQUANT assays(Only for Reference)

Molecular Weight	513.61
Formula	C27H27N7O2S
CAS No.	1138549-36-6

Storage

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

Solubility Information

DMSO: < 1 mg/mL

H2O: 5.1 mg/mL (10 mM), when pH is adjusted to 7 with HCl. Sonication is recommended.

References and Literature

1. Drygin D, et al, Cancer Res, 2011, 71(4), 1418-1430. 2. Li, Dingfeng, Juan Zhang, Ming Wang, Xiaohui Li, Huarui Gong, Huiping Tang, Lin Chen, Lili Wan, and Qiang Liu. Activity dependent LoNA regulates translation by coordinating rRNA transcription and methylation[J]. Nature communications. 2018 Apr 30;9(1):1726.

Citations

1. Li, Dingfeng, Juan Zhang, Ming Wang, Xiaohui Li, Huarui Gong, Huiping Tang, Lin Chen, Lili Wan, and Qiang Liu. Activity dependent LoNA regulates translation by coordinating rRNA transcription and methylation. Nature Communications. 2018, 9(1): 1-14 2. Fu Y, Liu Y, Wen T, et al. Real-time imaging of RNA polymerase I activity in living human cells. Journal of Cell Biology. 2022, 222(1): e202202110. 3. Liu T, Wu Y, Qin L, et al.Nonselective Intercalation of G-Quadruplex-Targeting Ligands into Double-Stranded DNA Quantified by Single-Molecule Stretching.The Journal of Physical Chemistry B.2023 4. Zhang Y, Cheng Y, Luo Q, et al.Distinguishing G-Quadruplexes Stabilizer and Chaperone for c-MYC Promoter G-Quadruplexes through Single-Molecule Manipulation.Journal of the American Chemical Society.2024

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Inhibitor Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library Bioactive Compound Library DNA Damage & Repair Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CX-5461 1138549-36-6 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis Inhibitor CX 5461 CX5461 inhibit inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.