2. PROTAC Vitamin D Related/Nuclear Receptor Autophagy
  3. AUTOTACs Estrogen Receptor/ERR Autophagy
  4. PHTPP-1304

PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.

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PHTPP-1304

PHTPP-1304 Chemische Struktur

CAS. Nr. : 2410081-60-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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PHTPP-1304 Related Antibodies

Top Publications Citing Use of Products

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Beschreibung

PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ[1].

IC50 & Target[1]

ERβ

2 nM (DC50)

In Vitro

PHTPP-1304 (0.5-10 μM, 24 h) induces the formation of p62+ERβ+ puncta that are affected by autophagic flux in a dose-dependent manner in ACHN cells[1].
PHTPP-1304 (0.01-100 μM) has cytotoxicity against ACHN cells (IC50 = 3.3 μM), and can effectively inhibit the migration of cancer cells[1].
PHTPP-1304 (0.5 μM, 24 h) exhibits a 10-fold stronger inhibitory effect on ERβ downstream signaling (EGFR, p-ERK/ERK, p-Akt/Akt) in estrogen (E2)-stimulated LNCaP cells compared to PHTPP alone[1].

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

PHTPP-1304 Related Antibodies

Western Blot Analysis[1]

Cell Line: LNCaP cells with or without E2 (10 nM)
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Inhibited ERβ signaling 10-folds more efficiently than its TBL as determined by the levels of EGFR, p-ERK/ERK and p-Akt/Akt in E2-stimulated LNCaP cells.
Molekulargewicht

944.96

Formel

C51H50F6N4O7
CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O[C@H](CNCCOCCOCCOC1=CC=C(C2=C3N(C(C(F)(F)F)=CC(C(F)(F)F)=N3)N=C2C4=CC=CC=C4)C=C1)COC5=CC(OCCCC6=CC=CC=C6)=C(OCC7=CC=CC=C7)C=C5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 110 mg/mL (116.41 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 1.0582 mL 5.2912 mL 10.5825 mL
5 mM 0.2116 mL 1.0582 mL 2.1165 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 (protect from light, stored under nitrogen). 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

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In Vivo Dissolution Calculator
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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 (protect from light, stored under nitrogen). 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 1.0582 mL 5.2912 mL 10.5825 mL 26.4561 mL
5 mM 0.2116 mL 1.0582 mL 2.1165 mL 5.2912 mL
10 mM 0.1058 mL 0.5291 mL 1.0582 mL 2.6456 mL
15 mM 0.0705 mL 0.3527 mL 0.7055 mL 1.7637 mL
20 mM 0.0529 mL 0.2646 mL 0.5291 mL 1.3228 mL
25 mM 0.0423 mL 0.2116 mL 0.4233 mL 1.0582 mL
30 mM 0.0353 mL 0.1764 mL 0.3527 mL 0.8819 mL
40 mM 0.0265 mL 0.1323 mL 0.2646 mL 0.6614 mL
50 mM 0.0212 mL 0.1058 mL 0.2116 mL 0.5291 mL
60 mM 0.0176 mL 0.0882 mL 0.1764 mL 0.4409 mL
80 mM 0.0132 mL 0.0661 mL 0.1323 mL 0.3307 mL
100 mM 0.0106 mL 0.0529 mL 0.1058 mL 0.2646 mL
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PHTPP-1304 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:

PHTPP-13042410081-60-4PHTPP1304PHTPP 1304AUTOTACsEstrogen Receptor/ERRAutophagyAUTOphagy-TArgeting ChimerasAUTOTACACHN cellsLNCaP cellsMCF-7 cellsautophagyInhibitorinhibitorinhibit

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