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

PROTAC PIN1 degrader-2 is a PROTAC PIN1 degrader. PROTAC PIN1 degrader-2 reduces PIN1-mediated oncogene expression, upregulates PIN1-inhibited tumor suppressor genes, and exerts killing effects on cancer cells. PROTAC PIN1 degrader-2 inhibits tumor growth in breast cancer mouse xenograft models. PROTAC PIN1 degrader-2 can be used for the research of breast cancer.
(Pink: PIN1 ligand (HY-186219); Blue: Cereblon ligand (HY-103596); Black: linker).

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

PROTAC PIN1 degrader-2-1

PROTAC PIN1 degrader-2-1 Chemical Structure

CAS No. : 3083422-10-7

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PROTAC PIN1 degrader-2-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC PIN1 degrader-2 is a PROTAC PIN1 degrader. PROTAC PIN1 degrader-2 reduces PIN1-mediated oncogene expression, upregulates PIN1-inhibited tumor suppressor genes, and exerts killing effects on cancer cells. PROTAC PIN1 degrader-2 inhibits tumor growth in breast cancer mouse xenograft models. PROTAC PIN1 degrader-2 can be used for the research of breast cancer[1]. (Pink: PIN1 ligand (HY-186219); Blue: Cereblon ligand (HY-103596); Black: linker).

In Vitro

PROTAC PIN1 degrader-2 (compound A1) (2.2 μM-20 μM; 0-36 h) specifically degrades PIN1 protein in MCF-7 breast cancer cells with a DC50 of 269 nM, achieving 90% degradation at 2.2 μM and reaching maximum degradation at 12 hours post-treatment[1].
PROTAC PIN1 degrader-2 (2.2 μM-20 μM; 0-36 h) degrades PIN1 protein in PATU-8988t pancreatic cancer cells, with effective degradation at 2.2 μM and a Hook effect occurring at 20 μM[1].
PROTAC PIN1 degrader-2 (0.08 μM-20 μM; 72 h) inhibits the viability of MCF-7 breast cancer cells, and this inhibitory activity is enhanced in an additive manner when combined with RO3306[1].
PROTAC PIN1 degrader-2 (0.08 μM-20 μM; 72 h) inhibits the viability of PATU-8988t pancreatic cancer cells, and this inhibitory activity is enhanced in an additive manner when combined with RO3306[1].

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

PROTAC PIN1 degrader-2-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MCF-7 breast cancer cells
Concentration: 2.2; 6.7; 20 μM
Incubation Time: 0; 6; 12; 18; 24; 36 h
Result: Significantly reduced PIN1 protein levels.
Achieved 90% degradation efficiency at 2.2 μM.
Exhibited a DC50 value of 269 nM for PIN1 degradation.
Reached peak PIN1 degradation at 12 hours, followed by protein recovery after 12 hours.

Cell Viability Assay[1]

Cell Line: MCF-7 breast cancer cells
Concentration: 0.08; 0.25; 0.74; 2.22; 6.66; 20 μM
Incubation Time: 72 h
Result: Inhibited MCF-7 cell viability in a concentration-dependent manner when used alone.
Showed additive cell viability inhibition effect when combined with 1 μM or 5 μM RO3306, with significantly stronger inhibition than the degrader alone at equivalent concentrations.

Cell Viability Assay[1]

Cell Line: PATU-8988t pancreatic cancer cells
Concentration: 0.08; 0.25; 0.74; 2.22; 6.66; 20 μM
Incubation Time: 72 h
Result: Inhibited PATU-8988t cell viability in a concentration-dependent manner when used alone.
Showed additive cell viability inhibition effect when combined with 1 μM or 5 μM RO3306, with significantly stronger inhibition than the degrader alone at equivalent concentrations.
In Vivo

PROTAC PIN1 degrader-2 (compound A1) (50 mg/kg; i.p.; every other day; 20 days) significantly inhibits tumor growth in a mouse MCF-7 breast cancer xenograft model, with no observed toxicity over 20 days[1].

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

Animal Model: BALB/c-Nude mice (female, 5 weeks old, MCF-7 cell xenograft model with estradiol pre-treatment)[1]
Dosage: 50 mg/kg
Administration: i.p.; every other day; 20 days
Result: Inhibited tumor growth significantly compared to vehicle control group after 20 days.
Maintained stable body weight and exhibited normal behavior with no observed toxicity.
Molecular Weight

640.10

Formula

C28H34ClN3O10S
CAS No.
SMILES

O=C(CCCOC1=CC=CC(C(N2C3C(NC(CC3)=O)=O)=O)=C1C2=O)OCC(C)(CN(C4CCS(=O)(C4)=O)C(CCl)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC PIN1 degrader-2-1 Related Classifications

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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-2-13083422-10-7PROTACsPIN1peptidylprolyl cis/trans isomerase, NIMA-interacting 1MCF-7 breast cancer cellsliver canceracute myeloid leukemiamultiple myelomapancreatic cancercolon cancerbreast cancerlung cancerprostate cancerInhibitorinhibitorinhibit

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