跳转至内容
Merck
CN

SML2601

dTAG-13

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

别名:

(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

登录 查看组织和合同定价。

选择尺寸

变更视图

关于此项目

经验公式(希尔记法):
C57H68N4O15
化学文摘社编号:
分子量:
1049.17
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
技术服务
需要帮助?我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助


产品名称

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

InChI

1S/C57H68N4O15/c1-7-37(36-32-47(71-4)52(73-6)48(33-36)72-5)54(65)60-29-14-12-19-41(60)57(68)76-43(25-22-35-23-26-44(69-2)46(31-35)70-3)38-17-10-11-20-42(38)75-34-50(63)58-28-13-8-9-15-30-74-45-21-16-18-39-51(45)56(67)61(55(39)66)40-24-27-49(62)59-53(40)64

InChI key

BJFBRLAWLPZOMJ-QHVFGHLPSA-N

Biochem/physiol Actions

Degradation tag (dTAG) system heterobifunctional degrader of FKBP12(F36V) fusions by bridging them with CRBN for ubiquitination.
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.


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our 文件 section.

如需帮助,请联系 客户支持

已有该产品?

在文件库中查找您最近购买产品的文档。

访问文档库



Behnam Nabet et al.
Nature chemical biology, 14(5), 431-441 (2018-03-28)
Dissection of complex biological systems requires target-specific control of the function or abundance of proteins. Genetic perturbations are limited by off-target effects, multicomponent complexity, and irreversibility. Most limiting is the requisite delay between modulation to experimental measurement. To enable the
Transcription control by the ENL YEATS domain in acute leukaemia
Erb MA, Scott TG, Li BE, et al.
Nature, 543(7644), 270-274 (2017)
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