2. PROTAC
  3. Ligands for E3 Ligase
  4. (S,R,S)-AHPC

(S,R,S)-AHPC  (Synonyms: VH032-NH2; VHL ligand 1)

Cat. No.: HY-125845 Pureza: 99.09%
COA
SDS
Instrucciones de manejo Technical Support

(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC 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.

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(S,R,S)-AHPC

(S,R,S)-AHPC Estructura química

No. CAS : 1448297-52-6

Tamaño Precio Stock Cantidad
Muestra gratis (0.1 - 0.2 mg)   Solicite ahora  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
100 mg En stock
500 mg En stock
1 g En stock
5 g En stock
10 g   Obtener un presupuesto  
50 g   Obtener un presupuesto  

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Revisión del cliente

Based on 2 publication(s) in Google Scholar

Other Forms of (S,R,S)-AHPC:

(S,R,S)-AHPC Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE (S,R,S)-AHPC

Ver todos los productos específicos de isoformas Ligands for E3 Ligase:

Ver todas las isoformas
von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B

  • Actividad biológica

  • Pureza y Documentación

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Descripciòn

(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC 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[1].

IC50 & Target[1]

VHL

 

Cellular Effect
Cell Line Type Value Description References
HCC827 IC50
> 10 μM
Compound: VHL-L
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 31951960]
HCT-116 IC50
> 50 μM
Compound: VHL
Antiproliferative activity against human HCT-116 cells expressing wildtype ATM incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HCT-116 cells expressing wildtype ATM incubated for 72 hrs by CCK8 assay
[PMID: 38325007]
LoVo IC50
> 50 μM
Compound: VHL
Antiproliferative activity against ATM deficient human LoVo cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against ATM deficient human LoVo cells incubated for 72 hrs by CCK8 assay
[PMID: 38325007]
In Vitro

The VHL protein is a substrate recognition subunit of two ubiquitously expressed and biologically important Cullin RING E3 ubiquitin ligase complexes. VHL is one of the most popular E3 ligases being recruited by bifunctional Proteolysis-targeting chimeras (PROTACs) to induce ubiquitination and subsequent proteasomal degradation of a target protein[1].

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

(S,R,S)-AHPC Related Antibodies
Peso molecular

430.56

Fòrmula

C22H30N4O3S
No. CAS
Appearance

Solid

Color

White to light yellow

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (232.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (11.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3226 mL 11.6128 mL 23.2256 mL
5 mM 0.4645 mL 2.3226 mL 4.6451 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 99.13%

SDS (393 KB)

COA (250 KB) HNMR (134 KB) RP-HPLC (235 KB) LCMS (89 KB)

Instrucciones de manejo (2659 KB)
Referencias

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
H2O / DMSO 1 mM 2.3226 mL 11.6128 mL 23.2256 mL 58.0639 mL
5 mM 0.4645 mL 2.3226 mL 4.6451 mL 11.6128 mL
10 mM 0.2323 mL 1.1613 mL 2.3226 mL 5.8064 mL
DMSO 15 mM 0.1548 mL 0.7742 mL 1.5484 mL 3.8709 mL
20 mM 0.1161 mL 0.5806 mL 1.1613 mL 2.9032 mL
25 mM 0.0929 mL 0.4645 mL 0.9290 mL 2.3226 mL
30 mM 0.0774 mL 0.3871 mL 0.7742 mL 1.9355 mL
40 mM 0.0581 mL 0.2903 mL 0.5806 mL 1.4516 mL
50 mM 0.0465 mL 0.2323 mL 0.4645 mL 1.1613 mL
60 mM 0.0387 mL 0.1935 mL 0.3871 mL 0.9677 mL
80 mM 0.0290 mL 0.1452 mL 0.2903 mL 0.7258 mL
100 mM 0.0232 mL 0.1161 mL 0.2323 mL 0.5806 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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(S,R,S)-AHPC 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:

(S,R,S)-AHPC1448297-52-6VH032-NH2 VHL ligand 1VHL ligand1VHL ligand 1VHL ligand-1Ligands for E3 LigaseE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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Nombre del producto:
(S,R,S)-AHPC
Cat. No.:
HY-125845
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