1. PROTAC
  2. E3 Ligase Ligand-Linker Conjugate
  3. Thalidomide-NH-C6-NH-Boc

Thalidomide-NH-C6-NH-Boc 

Cat. No.: HY-130854
Handling Instructions

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).

For research use only. We do not sell to patients.

Thalidomide-NH-C6-NH-Boc Chemical Structure

Thalidomide-NH-C6-NH-Boc Chemical Structure

CAS No. : 2093536-13-9

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Description

Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A)[1].

IC50 & Target[1]

Cereblon

 

In Vitro

MI-389 (0-1 μM; 72 hours) decreases cell growth with an EC50 value of 21.3 nM, which is comparable to the cellular potency of sunitinib (EC50=17.3 nM)[1].
MI-389 (0-500 nM; 72 hours) leads to GSPT1 destabilization fastly as a dosepdependent manner. It shows a complete GSPT1 depletion at 100 nM[1].

Cell Viability Assay[1]

Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1
Concentration: 0-1 μM
Incubation Time: 72 hours
Result: Outperform decreased-antiproliferative effect than sunitinib

Western Blot Analysis[1]

Cell Line: Kasumi-1 cells (a c-KIT dependent acute myeloid leukemia (AML) cell line); GIST-T1
Concentration: 1 nM, 5 nM, 10 nM, 50 nM, 100 nM, 500 nM
Incubation Time: 4 hours
Result: Decreased GSPT-1 protein expression.
Molecular Weight

472.53

Formula

C₂₄H₃₂N₄O₆

CAS No.

2093536-13-9

SMILES

O=C(OC(C)(C)C)NCCCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Thalidomide-NH-C6-NH-BocE3 Ligase Ligand-Linker ConjugateMI389PROTACKasumi-1leukemiaAMLT-AMLCCRF-CEMJURKATMOLT4Inhibitorinhibitorinhibit

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Thalidomide-NH-C6-NH-Boc
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HY-130854
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