(Rac)-P1D-34
Based on 1 Customer Validation
(Rac)-P1D-34 is a Pin1 PROTAC degrader that recruits cereblon, with a DC50 of 177 nM. (Rac)-P1D-34 induces Pin1 degradation via proteasome- and ubiquitin-like modification-dependent pathways. (Rac)-P1D-34 upregulates ROS and DNA damage, downregulates the UPR pathway, and inhibits leukemia cell proliferation; it also sensitizes drug-resistant acute myeloid leukemia cells to Venetoclax (ABT-199) (HY-15531) by downregulating Mcl-1 levels. (Rac)-P1D-34 can be used in the research of acute myeloid leukemia.
(Pink: PIN1 ligand (HY-171442); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W014883)).
For research use only. We do not sell to patients.
- Purity : 99.45%
- CAS No.: 2957895-04-2
- Formula: C40H59ClN6O9S
- Molecular Weight:835.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Mcl-1 |
Pin1 177 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | DC50 |
177 nM
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Pin1 degradation in human MV-4-11 acute myeloid leukemia cells assessed via immunoblot analysis after 24 h incubation.
Pin1 degradation in human MV-4-11 acute myeloid leukemia cells assessed via immunoblot analysis after 24 h incubation.
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38550694 |
| MV4-11 | IC50 |
2248 nM
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Antiproliferative activity against human MV-4-11 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
Antiproliferative activity against human MV-4-11 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
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38550694 |
| MOLM-13 | IC50 |
3984 nM
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Antiproliferative activity against human MOLM-13 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
Antiproliferative activity against human MOLM-13 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
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38550694 |
| HL-60 | IC50 |
3925 nM
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Antiproliferative activity against human HL-60 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
Antiproliferative activity against human HL-60 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
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38550694 |
| THP-1 | IC50 |
7669 nM
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Antiproliferative activity against human THP-1 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
Antiproliferative activity against human THP-1 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
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38550694 |
| Kasumi 1 | IC50 |
5389 nM
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Antiproliferative activity against human Kasumi-1 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
Antiproliferative activity against human Kasumi-1 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
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38550694 |
| OCI-AML-3 | IC50 |
6758 nM
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Antiproliferative activity against human OCI-AML3 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
Antiproliferative activity against human OCI-AML3 acute myeloid leukemia cells assessed as reduction in cell viability after 72 h incubation.
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38550694 |
In Vitro
(Rac)-P1D-34 (0.156-20 μM; 2-24 h) induces dose- and time-dependent degradation of Pin1 in MV-4-11 acute myeloid leukemia cells via proteasome- and ubiquitin-like modification-dependent mechanisms, with a DC50 of 177 nM and a maximum degradation rate of 95%[1].
(Rac)-P1D-34 (72 h) potently inhibits the proliferation of AML cell lines including MV-4-11, MOLM-13, HL-60, THP-1, Kasumi-1, BDCM and OCI-AML3 via a Pin1 degradation-dependent manner, with IC50 values ranging from 2248 nM to 7669 nM[1].
(Rac)-P1D-34 (compound 1) inhibits the proliferation of acute myeloid leukemia MV-4-11 cells after 72 h, with an IC50 of 2248 nM[2].
(Rac)-P1D-34 (72 h) inhibits the proliferation of acute myeloid leukemia cell lines MOLM-13, HL-60, THP-1, Kasumi-1, BDCM and OCI-AML3, with IC50 values ranging from 3925 nM to 7669 nM[2].
(Rac)-P1D-34 (2-20 μM; 24 h) induces 67.40% degradation of Pin1 protein in acute myeloid leukemia MV-4-11 cells at a concentration of 2 μM, and the degradation rate reaches 99.12% at 20 μM after 24 h of incubation[2].
(Rac)-P1D-34 (0.625-10 μM; 24 h) induces dose-dependent apoptosis and G1/S cell cycle arrest in MV-4-11 and MOLM-13 acute myeloid leukemia (AML) cells, and downregulates Pin1 substrate proteins Cyclin D1, pRb, Mcl-1, Akt and c-Myc[1].
(Rac)-P1D-34 (0.625-10 μM; 72 h) acts synergistically with Venetoclax (ABT-199) (HY-15531) to inhibit proliferation and induce apoptosis in ABT-199-resistant Kasumi-1 and MV-4-11 R AML cells, with HSA synergy scores of 15.645 and 26.391, respectively[1].
(Rac)-P1D-34 (0-10000 nM; 24-72 h) synergizes with 2-Deoxy-D-glucose (2-DG) (HY-13966) to inhibit proliferation and induce apoptosis of MV-4-11 acute myeloid leukemia (AML) cells, with a HSA synergy score of 8.564[1].
(Rac)-P1D-34 (5 μM; 24-36 h) induces reactive oxygen species (ROS)-dependent DNA damage and apoptosis in MV-4-11 acute myeloid leukemia (AML) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 acute myeloid leukemia (AML) cells
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Concentration:0.156, 0.312, 0.625, 1.25, 2.5, 5, 10, 20 μM
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Incubation Time:2, 4, 8, 12, 16, 18, 20, 22, 24 h
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Result:Induced dose-dependent Pin1 degradation with a DC50 of 177 nM and a maximum degradation (Dmax) of 95%.
Achieved more than 50% Pin1 degradation after 16 h of exposure to 5 μM, with 79% degradation at 24 h.
Accelerated Pin1 degradation when co-treated with cycloheximide, with significant decreases observed at 10 h.
Had its Pin1 degradation effect blocked by pre-treatment with thalidomide, Sulfopin, MLN4924, or MG132.
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Cell Line:MV-4-11
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Concentration:serial dilutions
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Incubation Time:72 h
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Result:Inhibited MV-4-11 cell proliferation with an IC50 of 2248 nM.
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Cell Line:MV-4-11
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Concentration:2 μM, 20 μM
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Incubation Time:24 h
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Result:Induced 67.40% degradation of Pin1 protein at 2 μM after 24 h.
Induced 99.12% degradation of Pin1 protein at 20 μM after 24 h.
Chemical Information
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CAS No. 2957895-04-2
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Appearance Solid
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Molecular Weight 835.45
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Formula C40H59ClN6O9S
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Color Light yellow to yellow
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SMILES
O=C1NC(C(CC1)N2C(C3=CC=C(NCCCCCCCCCCCCNC(CCC(NCC(C)(CN(C4CCS(=O)(C4)=O)C(CCl)=O)C)=O)=O)C=C3C2=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 : 100 mg/mL (119.70 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)
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1970 mL | 5.9848 mL | 11.9696 mL | 29.9240 mL |
| 5 mM | 0.2394 mL | 1.1970 mL | 2.3939 mL | 5.9848 mL | |
| 10 mM | 0.1197 mL | 0.5985 mL | 1.1970 mL | 2.9924 mL | |
| 15 mM | 0.0798 mL | 0.3990 mL | 0.7980 mL | 1.9949 mL | |
| 20 mM | 0.0598 mL | 0.2992 mL | 0.5985 mL | 1.4962 mL | |
| 25 mM | 0.0479 mL | 0.2394 mL | 0.4788 mL | 1.1970 mL | |
| 30 mM | 0.0399 mL | 0.1995 mL | 0.3990 mL | 0.9975 mL | |
| 40 mM | 0.0299 mL | 0.1496 mL | 0.2992 mL | 0.7481 mL | |
| 50 mM | 0.0239 mL | 0.1197 mL | 0.2394 mL | 0.5985 mL | |
| 60 mM | 0.0199 mL | 0.0997 mL | 0.1995 mL | 0.4987 mL | |
| 80 mM | 0.0150 mL | 0.0748 mL | 0.1496 mL | 0.3740 mL | |
| 100 mM | 0.0120 mL | 0.0598 mL | 0.1197 mL | 0.2992 mL |
(Rac)-P1D-34 Related Classifications
HY-171334 Related Classifications
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