2. PROTAC
  3. Ligands for E3 Ligase
  4. SJPYT-195

SJPYT-195 is a cytotoxic GSPT1 degrader and can be used for PROTAC synthesis.

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

SJPYT-195 Chemical Structure

SJPYT-195 Chemical Structure

CAS No. : 2973762-16-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 587 In-stock
Solution
10 mM * 1 mL in DMSO USD 587 In-stock
Solid
5 mg USD 400 In-stock
10 mg USD 690 In-stock
25 mg USD 1450 In-stock
50 mg USD 2460 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

SJPYT-195 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SJPYT-195 is a cytotoxic GSPT1 degrader and can be used for PROTAC synthesis[1].

In Vitro

SJPYT-195 (24 h) potently and efficaciously reduces endogenous PXR (pregnane X receptor) protein in the colorectal SNU-C4 cell line (SNU-C4 3xFLAG-PXR KI cells), with a half maximal degradation concentration (DC50) of 310 ± 130 nM and maximum degradation efficacy (DMax) of 85 ± 1%[1].
SJPYT-195 reduces PXR protein through the degradation of GSPT1[1].

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

SJPYT-195 Related Antibodies
Molecular Weight

666.68

Formula

C35H34N6O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C)N(C2=CC(OC)=CC=C2OC)N=N1)NC3=CC(OC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=CC(C(C)(C)C)=C3
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 : 50 mg/mL (75.00 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 1.5000 mL 7.4999 mL 14.9997 mL
5 mM 0.3000 mL 1.5000 mL 2.9999 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.

  • Molarity Calculator

  • Dilution Calculator

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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (3.12 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

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

    Solubility: ≥ 1.67 mg/mL (2.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
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.
Purity & Documentation

Purity: 99.41%

COA (250 KB) HNMR (307 KB) LCMS (95 KB)

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
DMSO 1 mM 1.5000 mL 7.4999 mL 14.9997 mL 37.4993 mL
5 mM 0.3000 mL 1.5000 mL 2.9999 mL 7.4999 mL
10 mM 0.1500 mL 0.7500 mL 1.5000 mL 3.7499 mL
15 mM 0.1000 mL 0.5000 mL 1.0000 mL 2.5000 mL
20 mM 0.0750 mL 0.3750 mL 0.7500 mL 1.8750 mL
25 mM 0.0600 mL 0.3000 mL 0.6000 mL 1.5000 mL
30 mM 0.0500 mL 0.2500 mL 0.5000 mL 1.2500 mL
40 mM 0.0375 mL 0.1875 mL 0.3750 mL 0.9375 mL
50 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7500 mL
60 mM 0.0250 mL 0.1250 mL 0.2500 mL 0.6250 mL
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SJPYT-195 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:

SJPYT-1952973762-16-0SJPYT195SJPYT 195Ligands for E3 LigaseE3 ligase-recruiting MoietyanticancerCRBNGSPT1PXRpregnane X receptorPROTACInhibitorinhibitorinhibit

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