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  3. E3 Ligase Ligand-Linker Conjugates Drug Derivative
  4. Tz-Thalidomide

Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research.

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

Tz-Thalidomide

Tz-Thalidomide Chemical Structure

CAS No. : 2087490-42-2

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Based on 1 publication(s) in Google Scholar

Other Forms of Tz-Thalidomide:

Tz-Thalidomide Related Antibodies

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View All E3 Ligase Ligand-Linker Conjugates Isoform Specific Products:

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von Hippel-Lindau (VHL) MDM2 Cereblon cIAP1 Aryl Hydrocarbon Receptor TRIM21

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Description

Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research[1].

IC50 & Target[1]

Cereblon

 

In Vitro

Tz-Thalidomide exhibits extremely weak binding to the bromodomains of BRD4-1 and BRD4-2, with IC50 values of 46.25 μM and 62.55 μM, respectively[1].
Tz-Thalidomide (30 μM; 30 min) exhibits extremely weak inhibitory activity against ERK2, showing only 46% inhibition at a concentration of 30 μM[1].
Combined with JQ1-TCO, Tz-Thalidomide (0.1-10 μM; 18 h) induces concentration-dependent degradation of BRD4 in HeLa cells, with complete degradation achieved at concentrations of 10 μM and 3 μM after 18 h of incubation[1].
Combination treatment with Tz-Thalidomide (10 μM; 1-24 h) and JQ1-TCO induces time-dependent degradation of BRD4 in HeLa cells, with complete degradation observable after 24 h of incubation[1].
Combination treatment with Tz-Thalidomide (10 μM; 1-24 h) and Probe 1 induces time-dependent degradation of ERK1/2 in A375 cells, with complete degradation observable after 16 h of incubation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tz-Thalidomide Related Antibodies

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0.1-10 μM
Incubation Time: 18 h
Result: Completely degraded BRD4 at 10 μM and 3 μM.
Partially degraded BRD4 at 1 μM and 0.3 μM.
Did not degrade BRD4 at 0.1 μM.
Did not affect BRD4 levels when administered alone.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 10 μM
Incubation Time: 1-24 h
Result: Showed no change in BRD4 levels up to 8 h after addition.
Decreased BRD4 levels visibly by 16 h.
Resulted in undetectable (100% degraded) BRD4 levels by 24 h.

Western Blot Analysis[1]

Cell Line: A375 cells
Concentration: 10 μM
Incubation Time: 1-24 h
Result: Partially degraded ERK1/2 by 4 h after addition.
Completely degraded ERK1/2 by 16 h.
Molecular Weight

571.58

Formula

C29H29N7O6
CAS No.
Appearance

Solid

Color

Pink to red

SMILES

O=C(CCCCCOC1=C(C(N(C2CCC(NC2=O)=O)C3=O)=O)C3=CC=C1)NCC(C=C4)=CC=C4C5=NN=C(C)N=N5
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Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (87.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7495 mL 8.7477 mL 17.4954 mL
5 mM 0.3499 mL 1.7495 mL 3.4991 mL
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* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7495 mL 8.7477 mL 17.4954 mL 43.7384 mL
5 mM 0.3499 mL 1.7495 mL 3.4991 mL 8.7477 mL
10 mM 0.1750 mL 0.8748 mL 1.7495 mL 4.3738 mL
15 mM 0.1166 mL 0.5832 mL 1.1664 mL 2.9159 mL
20 mM 0.0875 mL 0.4374 mL 0.8748 mL 2.1869 mL
25 mM 0.0700 mL 0.3499 mL 0.6998 mL 1.7495 mL
30 mM 0.0583 mL 0.2916 mL 0.5832 mL 1.4579 mL
40 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0935 mL
50 mM 0.0350 mL 0.1750 mL 0.3499 mL 0.8748 mL
60 mM 0.0292 mL 0.1458 mL 0.2916 mL 0.7290 mL
80 mM 0.0219 mL 0.1093 mL 0.2187 mL 0.5467 mL
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Tz-Thalidomide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tz-Thalidomide2087490-42-2E3 Ligase Ligand-Linker ConjugatesDrug DerivativeDrug derivativeA375 cellsERK1/2CereblonBRD4cancerCRBNE3 ubiquitin ligasebromodomainsproteolysis targeting chimeraHeLa cellsInhibitorinhibitorinhibit

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