Tz-Thalidomide
Based on 1 Customer Validation
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.
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- Purity: 98.60%
- CAS No.: 2087490-42-2
- 화학식: C29H29N7O6
- 분자량:571.58
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All E3 Ligase Ligand-Linker Conjugates Isoforms
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Biological Activity
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Cereblon |
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.
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Cell Line:HeLa cells
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Concentration:0.1-10 μM
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Incubation Time:18 h
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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.
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Cell Line:HeLa cells
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Concentration:10 μM
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Incubation Time:1-24 h
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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.
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Cell Line:A375 cells
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Concentration:10 μM
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Incubation Time:1-24 h
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Result:Partially degraded ERK1/2 by 4 h after addition.
Completely degraded ERK1/2 by 16 h.
Chemical Information
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CAS No. 2087490-42-2
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Appearance Solid
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분자량 571.58
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화학식 C29H29N7O6
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Color Pink to red
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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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (271 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
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 |
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| 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 |
Tz-Thalidomide Related Classifications
HY-101460 Related Classifications
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