2. PROTAC
  3. Ligands for E3 Ligase Molecular Glues
  4. PT-179

PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms.

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PT-179 Chemical Structure

PT-179 Chemical Structure

CAS No. : 2924858-25-1

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Based on 1 publication(s) in Google Scholar

PT-179 Related Antibodies

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Description

PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms[1].

In Vitro

SD40 is a degradation tag specific for PT-179. PT-179 (1-10 μM; 24 h) can induce eGFP degradation in HEK293T cells. The higher the evolution degree of the degron variant, the stronger the degradation efficiency of the corresponding tagged protein[1].

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

PT-179 Related Antibodies
Molecular Weight

343.33

Formula

C17H17N3O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC=C(N3CCOCC3)C=C2C(N1C4C(NC(CC4)=O)=O)=O
Shipping

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 : 125 mg/mL (364.08 mM; ultrasonic and warming and heat to 60°C; 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 2.9126 mL 14.5632 mL 29.1265 mL
5 mM 0.5825 mL 2.9126 mL 5.8253 mL
View the 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.

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Purity & Documentation

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 2.9126 mL 14.5632 mL 29.1265 mL 72.8162 mL
5 mM 0.5825 mL 2.9126 mL 5.8253 mL 14.5632 mL
10 mM 0.2913 mL 1.4563 mL 2.9126 mL 7.2816 mL
15 mM 0.1942 mL 0.9709 mL 1.9418 mL 4.8544 mL
20 mM 0.1456 mL 0.7282 mL 1.4563 mL 3.6408 mL
25 mM 0.1165 mL 0.5825 mL 1.1651 mL 2.9126 mL
30 mM 0.0971 mL 0.4854 mL 0.9709 mL 2.4272 mL
40 mM 0.0728 mL 0.3641 mL 0.7282 mL 1.8204 mL
50 mM 0.0583 mL 0.2913 mL 0.5825 mL 1.4563 mL
60 mM 0.0485 mL 0.2427 mL 0.4854 mL 1.2136 mL
80 mM 0.0364 mL 0.1820 mL 0.3641 mL 0.9102 mL
100 mM 0.0291 mL 0.1456 mL 0.2913 mL 0.7282 mL
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PT-179 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:

PT-1792924858-25-1PT179PT 179Ligands for E3 LigaseMolecular GluesE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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