2. PROTAC PI3K/Akt/mTOR
  3. PIN1 PROTACs
  4. PROTAC PIN1 degrader-1

PROTAC PIN1 degrader-1 is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer.
(Pink: PIN1 ligand (HY-168038); Blue: Cereblon ligand (HY-14658); Black: linker).

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

PROTAC PIN1 degrader-1

PROTAC PIN1 degrader-1 Chemical Structure

CAS No. : 3038591-59-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PROTAC PIN1 degrader-1:

PROTAC PIN1 degrader-1 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC PIN1 degrader-1 is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer[1]. (Pink: PIN1 ligand (HY-168038); Blue: Cereblon ligand (HY-14658); Black: linker).

IC50 & Target

PIN1[1]
Cellular Effect
Cell Line Type Value Description References
Huh-7 GI50
> 30 μM
Compound: D4
Antiproliferative activity against human Huh-7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human Huh-7 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 39229909]
MDA-MB-468 GI50
> 30 μM
Compound: D4
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 39229909]
PANC-1 GI50
> 30 μM
Compound: D4
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition incubated for 96 hrs by Cell-Titer Glo assay
[PMID: 39229909]
In Vitro

PROTAC PIN1 degrader-1 (compound D4) (24 h) potently and selectively induces on-target degradation of PIN1 protein in MDA-MB-468 cells with a DC50 of 18 nM and maximum degradation of 92.52%[1].
PROTAC PIN1 degrader-1 (96 h) does not exhibit significant antiproliferative activity in MDA-MB-468, PANC-1, or Huh-7 cancer cells, with a GI50 greater than 30 μM[1].

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

PROTAC PIN1 degrader-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MDA-MB-468, PANC-1, and Huh-7 human cancer cells
Concentration: serial concentrations
Incubation Time: 96 h
Result: Exhibited no meaningful antiproliferative activity, with a GI50 > 30 μM in all three tested cancer cell lines.
Molecular Weight

917.02

Formula

C51H52N10O7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=CN=C1C2(CC2)C(NC(CC(N=N3)=CN3C(C=C4)=CC=C4C(C=C5)=CC=C5C#N)C(NC(CC6)CCN6CCCCCOC7=CC=CC(C8=O)=C7C(N8C(CC9)C(NC9=O)=O)=O)=O)=O
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 : 100 mg/mL (109.05 mM; Need ultrasonic; 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 1.0905 mL 5.4524 mL 10.9049 mL
5 mM 0.2181 mL 1.0905 mL 2.1810 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.

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 1.0905 mL 5.4524 mL 10.9049 mL 27.2622 mL
5 mM 0.2181 mL 1.0905 mL 2.1810 mL 5.4524 mL
10 mM 0.1090 mL 0.5452 mL 1.0905 mL 2.7262 mL
15 mM 0.0727 mL 0.3635 mL 0.7270 mL 1.8175 mL
20 mM 0.0545 mL 0.2726 mL 0.5452 mL 1.3631 mL
25 mM 0.0436 mL 0.2181 mL 0.4362 mL 1.0905 mL
30 mM 0.0363 mL 0.1817 mL 0.3635 mL 0.9087 mL
40 mM 0.0273 mL 0.1363 mL 0.2726 mL 0.6816 mL
50 mM 0.0218 mL 0.1090 mL 0.2181 mL 0.5452 mL
60 mM 0.0182 mL 0.0909 mL 0.1817 mL 0.4544 mL
80 mM 0.0136 mL 0.0682 mL 0.1363 mL 0.3408 mL
100 mM 0.0109 mL 0.0545 mL 0.1090 mL 0.2726 mL
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PROTAC PIN1 degrader-1 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:

PROTAC PIN1 degrader-13038591-59-9PIN1PROTACspeptidylprolyl cis/trans isomerase, NIMA-interacting 1triple-negative breast cancer cellsPANC-1 cellsCRBN ligandE3 ubiquitin ligase complexpancreatic cancerHuh-7 cellsliver cancerMDA-MB-468 cellstriple-negative breast cancerInhibitorinhibitorinhibit

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