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商品編號


5047/10



品牌


Tocris



公司


Bio-Techne Corporation



公司分類(lèi)


Ligases



Size

10 mg

商品信息

Description:
Inhibitor of Bmi1/Ring1A; blocks histone H2A ubiquitination

Chemical Name:
2-(3-Pyridinylmethylene)-1
H
-Indene-1,3(2
H
)-dione

Purity:
≥99% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

Inhibitor of Bmi1/Ring1A, subunits of the polycomb repressive complex 1 (PRC1); inhibits self-ubiquitination (IC
50
= 3.9
μ
M) but does not increase cellular levels of either subunit. Prevents Bmi1/Ring1A-mediated ubiquitination and drug-induced degradation of topoisomerase 2
α
(Top2
α
). Also shown to inhibit the
in vitro
E3 ubiquitin ligase activity of RNF2 and a Bmi1/RNF2 complex, inhibiting H2A/H2AX ubiquitination. Blocks polycomb repressor complex (PRC) 1-mediated histone H2A ubiquitination
in vitro
and
in vivo
.



Compound Libraries

PRT 4165 is also offered as part of the
Tocris
creen Plus and
Tocris
creen Epigenetics Toolbox. Find out more about compound libraries available from
Tocris
.



Technical Data



M. Wt

235.24



Formula

C
15
H
9
NO
2




Storage

Store at +4°C



Purity

≥99% (HPLC)



CAS Number

31083-55-3



PubChem ID

207893



InChI Key

OMHZFEWYVFWVLI-UHFFFAOYSA-N



Smiles

O=C(C2=CC=CC=C2C3=O)/C3=CC1=CC=CN=C1



The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All
Tocris
products are intended for laboratory research use only.



Solubility Data




Solvent

Max Conc. mg/mL

Max Conc. mM



Solubility



1eq. HCl

1.18

5mM with gentle warming



DMSO

23.52

100



ethanol

2.35

10mM with gentle warming





Preparing Stock Solutions

The following data is based on the
product
molecular weight
235.24
. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.



Concentration / Solvent Volume / Mass

1 mg

5 mg

10 mg



1 mM

4.25 mL

21.25 mL

42.51 mL



5 mM

0.85 mL

4.25 mL

8.5 mL



10 mM

0.43 mL

2.13 mL

4.25 mL



50 mM

0.09 mL

0.43 mL

0.85 mL






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Product Datasheets


Certificate of Analysis / Product Datasheet


Safety Datasheet

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References

References are publications that support the products'
BIOLOG
ical activity.


Alchanati

et al
(2009) The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2
α
cleavage complex - a potentially new drug target. PLoS One
4
e8104 PMID: 19956605


Ismail

et al
(2013) A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. J.Biol.Chem.
288
26944 PMID: 23902761




Keywords: PRT 4165, supplier, PRT4165, E3, ubiquitin, ligase, inhibitors, inhibits, Bmi1, Ring1A, ubiquitination, ubiquitylation, topoisomerase, 2a, Top2a, Top2alpha, Top2α, polycomb, repressive, complex, 1, PRC1, RNF2, Bmi1/RNF2, Ubiquitin, E3, Ligases, Ubiquitin, E3, Ligases,
Tocris
Bioscience