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5.09265

CX-5461

≥97% (HPLC), powder, RNA polymerase inhibitor, Calbiochem®

Synonym(s):

RNA Polymerase I Inhibitor II, CX-5461, Pol I Inhibitor II, CX5461, 2-(4-Methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide

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Size/SKUAvailabilityPrice
10 mg
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$309.00

About This Item

Empirical Formula (Hill Notation):
C27H27N7O2S
CAS Number:
1138549-36-6
Molecular Weight:
513.61
MDL number:
MFCD21609261
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light

$309.00

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Product Name

RNA Polymerase I Inhibitor II, CX-5461,

assay

≥97% (HPLC)

Quality Segment

100

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

light beige

solubility

DMSO: 0.5 mg/mL, dilute acetic acid: 10 mg/mL

storage temp.

2-8°C

SMILES string

[s]1c2[n](c4nc(ccc4[c](c2C(=O)NCc6ncc(nc6)C)=O)N5CCN(CCC5)C)c3c1cccc3

InChI

1S/C27H27N7O2S/c1-17-14-29-18(15-28-17)16-30-26(36)23-24(35)19-8-9-22(33-11-5-10-32(2)12-13-33)31-25(19)34-20-6-3-4-7-21(20)37-27(23)34/h3-4,6-9,14-15H,5,10-13,16H2,1-2H3,(H,30,36)

InChI key

XGPBJCHFROADCK-UHFFFAOYSA-N

General description

A cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142, 113, 54, and 74 nM in HCT-116, A375, MIA PaCa-2, and BJ-hTert cells, respectively), but not Pol II-mediated c-myc transcription, by preventing TAF (TATA Binding Protein-/TBP-Associated Factor) SL1 and rDNA association, effectively inhibiting Pol I-dependent proliferation among 39 cancer cell lines (IC50<1 µM) in vitro. While Pol I inhibition by CX-5461 is shown to result in p53-dependent apoptosis in cancer cells of hematopoietic origin, cell death by CX-5461 treatment in solid tumors-derived A375 and MIA PaCa-2 cultures are primarily due to autophagy and senescence, but not apoptosis, induction. Shown to suppress A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion, as well as selectively induce p53-mediated cell death of Eμ-Myc lymphoma, but not normal B cells, in mice (50 mg/kg p.o.) in vivo.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Pol I multi-protein complex
Reversible: yes

Packaging

Packaged under inert gas

Other Notes

Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 602.
Bywater, M.J., et al. 2012. Cancer Cell22, 51.
Drygin, D., et al. 2011. Cancer Res71, 1418.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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This Item
557404M557403526529
RNA Polymerase I Inhibitor II, CX-5461

Sigma-Aldrich

509265

RNA Polymerase I Inhibitor II, CX-5461

RNA Polymerase III Inhibitor InSolution, &#8805;97%

Millipore

557404M

RNA Polymerase III Inhibitor

RNA Polymerase III Inhibitor RNA Polymerase III Inhibitor, CAS 577784-91-9, is a cell-permeable inhibitor of RNA Polymerase III (IC50= 27 and 32 &#181;M for human and S. cerevisiae RNA Pol III, respectively).

Sigma-Aldrich

557403

RNA Polymerase III Inhibitor

PIM-Kinase Inhibitor X, CX-6258 The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation &amp; Dephosphorylation applications.

Sigma-Aldrich

526529

PIM-Kinase Inhibitor X, CX-6258

description

-

description

InSolution, ≥97%

description

RNA Polymerase III Inhibitor, CAS 577784-91-9, is a cell-permeable inhibitor of RNA Polymerase III (IC50= 27 and 32 µM for human and S. cerevisiae RNA Pol III, respectively).

description

The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

assay

≥97% (HPLC)

assay

≥97% (HPLC)

assay

≥95% (HPLC)

assay

≥99% (HPLC)

form

powder

form

liquid

form

solid

form

powder

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

−70°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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