商品编号


6154



品牌


Tocris



公司


Bio-Techne Corporation



公司分类


Ligases



Size

5 mg

商品信息

Description:
(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells

Chemical Name:
(2
S
,4
R
)-1-((
S
)-2-(tert-butyl)-17-((
S
)-4-(4-chlorophenyl)-2,3,9-trimethyl-6
H
-thieno[3,2-
f
][1,2,4]triazolo[4,3-
a
][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-
N
-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Purity:
≥98% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (K
d
= 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 (DC
50
values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively). Exhibits potent cytotoxicity and antiproliferative effects in AML cell lines (pEC50 = 7.6 in Mv4;11 cells). Negative control cis MZ 1 also available.

PROTACs are bi-functional small molecules that harness the ubiquitin/proteasome system (UPS) to selectively and catalytically remove target proteins from cells.



Licensing Information

Sold under licence from the University of Dundee



External Portal Information

Chemicalprobes.org
is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MZ 1 is reviewed on the Chemical Probes website.



Technical Data



M. Wt

1002.64



Formula

C
49
H
60
ClN
9
O
8
S
2




Storage

Store at -20°C



Purity

≥98% (HPLC)



CAS Number

1797406-69-9



PubChem ID

122201421



InChI Key

PTAMRJLIOCHJMQ-PYNGZGNASA-N



Smiles

CC1=C(C2=C(N3C(C)=NN=C3[C@@H](N=C2C4=CC=C(C=C4)Cl)CC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C7=C(N=CS7)C)C=C6)=O)O)=O)=O)=O)S1)C



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



DMSO

100.26

100



ethanol

100.26

100





Preparing Stock Solutions

The following data is based on the
product
molecular weight
1002.64
. 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

1 mL

4.99 mL

9.97 mL



5 mM

0.2 mL

1 mL

1.99 mL



10 mM

0.1 mL

0.5 mL

1 mL



50 mM

0.02 mL

0.1 mL

0.2 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.


Zengerle

et al
(2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS.Chem.Biol
10
1770 PMID: 26035625


Gadd

et al
(2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. PMID: 28288108


Wurz

et al
(2017) A "
Click chemistry
platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. PMID: 28378579




Keywords: MZ 1, supplier, MZ1, PROTAC, Proteolysis, targeted, chimeras, Bromodomain, BRD2, BRD3, BRD4, BET, proteins, JQ1, VHL, E3, ubiquitin, ligase, HIF-alpha, HIF-a, HIF-α, Ubiquitin, E3, Ligases,
Tocris
Bioscience