Protein degrader 1 hydrochloride |
Catalog No.GC19302
One-Click Copy Product Info
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(S,R,S)-AHPC (VH032-NH2) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. Protein degrader 1 hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1448189-80-7
Sample solution is provided at 25 µL, 10mM.
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Protein degrader 1 hydrochloride is used in the synthesis of HaloPROTACs.
Small molecule-induced protein degradation is an attractive strategy for the development of chemical probes.Protein degraders have the power to abrogate all of the functions of a drug target at once, including scaffolding functions which are difficult to target with small molecule inhibitors. A novel class of PROTACs that incorporate small molecule VHL ligands to successfully degrade HaloTag7 fusion proteins is developed. HaloPROTACs will inspire the development of future PROTACs with more drug-like properties. In HEK 293 cellsstably expressing GFP-HaloTag7,24 hour treatment with HaloPROTAC1 leads to less than 20% degradation, the longer HaloPROTAC2 leads to nearly 70% degradation of GFP-Halotag7 at 2.5 uM.HaloPROTACs containing protein degrader 1 leads to nearly 70% degradation of GFP-HaloTag7, when sufficiently long linkers are used[1].
References:
[1]. Buckley DL, et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.ACS Chem Biol. 2015 Aug 21;10(8):1831-7.
| Cas No. | 1448189-80-7 | SDF | |
| Canonical SMILES | O=C([C@H](C[C@@H](O)C1)N1C([C@@H](N)C(C)(C)C)=O)NCC2=CC=C(C(SC=N3)=C3C)C=C2.Cl | ||
| Formula | C22H31ClN4O3S | M.Wt | 467.02 |
| Solubility | DMSO : 150 mg/mL (321.19 mM);Water : 50 mg/mL (107.06 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1412 mL | 10.7062 mL | 21.4124 mL |
| 5 mM | 428.2 μL | 2.1412 mL | 4.2825 mL |
| 10 mM | 214.1 μL | 1.0706 mL | 2.1412 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)