P1D-34
Based on 1 publication(s) in Google Scholar
P1D-34 is a potent PIN1 PROTAC degrader with a DC50 of 177 nM. P1D-34 induces PIN1 degradation in a proteasome- and ubiquitination-like modification-dependent manner, thereby increasing intracellular ROS levels, downregulating the unfolded protein response pathway, and inducing DNA damage, cell cycle arrest and apoptosis. P1D-34 can be used in studies related to acute myeloid leukemia.
(Pink: PIN1 ligand (HY-171442A); Blue: Cereblon ligand (HY-14658); Black: linker (HY-W014883)).
For research use only. We do not sell to patients.
- Formula: C40H59ClN6O9S
- Molecular Weight:835.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) P1D-34
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Biological Activity
Description
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 after 24 h incubation measured via immunoblot-based assay.
Pin1 degradation in human MV-4-11 acute myeloid leukemia cells after 24 h incubation measured via immunoblot-based assay.
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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
P1D-34 (0.156-20 μM; 2-24 h) degrades Pin protein in a time- and dose-dependent manner in MV-4-11 cells, with a DC50 of 177 nM[1].
P1D-34 (31.6 nM-31.6 μM; 72 h) inhibits cell proliferation in MV-4-11, MOLM-13, HL-60, THP-1, Kasumi-1, BDCM, and OCI-AML3 cells[1].
P1D-34 (0.625-10 μM; 24-36 h) induces apoptosis, causes G1/S cell cycle arrest, downregulates the protein expression of Cyclin D1, pRb, Rb, Mcl-1, Akt and c-Myc, increases reactive oxygen species (ROS) production, and upregulates γH2AX phosphorylation in MV-4-11 and MOLM-13 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
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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:Degraded Pin1 protein in a dose-dependent manner.
Degraded Pin1 protein in a time-dependent manner.
Increased the phosphorylation level of γH2AX and triggered DNA damage.
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Cell Line:MV-4-11, MOLM-13, HL-60, THP-1, Kasumi-1, BDCM, OCI-AML3
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Concentration:31.6 nM, 100 nM, 316 nM, 1 μM, 3.16 μM, 10 μM, 31.6 μM
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Incubation Time:72 h
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Result:Significantly inhibited the viability and proliferation of leukemia cell lines.
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Cell Line:MV-4-11, MOLM-13
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Concentration:2.5, 5, 10 μM
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Incubation Time:24 h
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Result:Significantly induced cell apoptosis.
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Cell Line:MV-4-11, MOLM-13
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Concentration:0.625, 1.25, 2.5, 5 μM
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Incubation Time:24 h
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Result:Caused cell cycle G1/S phase arrest.
Chemical Information
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Molecular Weight 835.45
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Formula C40H59ClN6O9S
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SMILES
O=C(NCC(C)(C)CN([C@H](CC1)CS1(=O)=O)C(CCl)=O)CCC(NCCCCCCCCCCCCNC2=CC3=C(C(N(C(CC4)C(NC4=O)=O)C3=O)=O)C=C2)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Pharmaceutics
Systematic Optimization of Proteolysis-Targeting Chimeras for PIN1 Enables Selective Degradation and Antitumor Activity In Vivo. [Abstract]2026 Feb 26;18(3):288. PMID: 41900774
Purity & Documentation
References
[1]. Shi Y, et al. Discovery of potent PROTAC degraders of Pin1 for the treatment of acute myeloid leukemia. Chemical science. 2024 Mar 27;15(13):5027-5035. [Content Brief]
[2]. Mohammed MH, et al. Therapeutic innovations: targeting ROS production in AML with natural and synthetic compounds. Naunyn-Schmiedeberg's archives of pharmacology. 2025 Sep;398(9):11387-11406. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
P1D-34 Related Classifications
HY-171334A Related Classifications
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