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SML2601

Sigma-Aldrich

dTAG-13

≥98% (HPLC), powder, degradation tag  (dTAG) system

Synonym(s):

(2S)-(1R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)hexyl)amino)-2-oxoethoxy)phenyl)propyl 1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate, d-TAG-13

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About This Item

Empirical Formula (Hill Notation):
C57H68N4O15
CAS Number:
Molecular Weight:
1049.17
UNSPSC Code:
12352200
NACRES:
NA.77

product name

dTAG-13, ≥98% (HPLC)

ligand

thalidomide

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

SMILES string

O=C(O[C@@H](C1=C(C=CC=C1)OCC(NCCCCCCOC2=C(C3=CC=C2)C(N(C3=O)C4CCC(NC4=O)=O)=O)=O)CCC5=CC=C(C(OC)=C5)OC)[C@@H]6CCCCN6C([C@H](C7=CC(OC)=C(C(OC)=C7)OC)CC)=O

Biochem/physiol Actions

dTAG-13 is a degradation tag (dTAG) system heterobifunctional degrader composed of an E3 ubiquitin ligase cereblon (CRBN)-binding thalidomide moiety and an FKBP12(F36V) mutant-specific ligand AP1867 void of affinity for endogenous (wild-type) FKBP12, allowing selective degradation of target proteins of interest when expressed as an FKBP12(F36V) in-frame fusion (by transgene expression or locus-specific knock-in) by bridging them with CRBN for ubiquitination. dTAG-13 is shown to potently degrade FKBP12F36V-MELK(sg3R) in MDA-MB-468 cells (100 nM for 4 hrs) as well as ENL-FKBP12F36V-HA, but not endogenous ENL, in MV4;1 cells (500 nM for 0.5-1 hrs).

Other Notes

Contains a mixture of diastereomers. This product has not been tested in cellular degradation assays.

Legal Information

Sold with permission under license from Dana Farber Cancer Institute.

related product

Product No.
Description
Pricing

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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MELK is not necessary for the proliferation of basal-like breast cancer cells
Huang HT, Seo HS, Zhang T, et al.
eLife, 6, e26693-e26693 (2017)
The dTAG system for immediate and target-specific protein degradation.
Nabet B, Roberts JM, Buckley DL, et al.
Nature Chemical Biology, 14(5), 431-441 (2018)
Michael A Erb et al.
Nature, 543(7644), 270-274 (2017-02-28)
Recurrent chromosomal translocations producing a chimaeric MLL oncogene give rise to a highly aggressive acute leukaemia associated with poor clinical outcome. The preferential involvement of chromatin-associated factors as MLL fusion partners belies a dependency on transcription control. Despite recent progress
Hai-Tsang Huang et al.
eLife, 6 (2017-09-20)
Thorough preclinical target validation is essential for the success of drug discovery efforts. In this study, we combined chemical and genetic perturbants, including the development of a novel selective maternal embryonic leucine zipper kinase (MELK) inhibitor HTH-01-091, CRISPR/Cas9-mediated MELK knockout
Transcription control by the ENL YEATS domain in acute leukaemia
Erb MA, Scott TG, Li BE, et al.
Nature, 543(7644), 270-274 (2017)

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