2. PROTAC Apoptosis
  3. PROTACs Bcl-2 Family Apoptosis
  4. PZ671

PZ671 is a potent Bcl-xL PROTAC degrader with an IC50 of 1.3 nM (MOLT-4 cells) and a DC50 of 0.9 nM (Bcl-xL). PZ671 induces apoptosis in MOLT-4 cells. PZ671 effectively inhibits tumor growth and rapidly reverses transient platelet counts reduction in MOLT-4 xenograft mice. PZ671 can be used for the research of cancer, such as small cell lung cancer (SCLC). (Structure Note: Pink: Bcl-xL ligand (HY-174878); Blue: E3 ligase Ligand (HY-138793); Black: linker; E3-linker (HY-174879))

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PZ671 Chemical Structure

PZ671 Chemical Structure

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PZ671 Related Antibodies

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Description

PZ671 is a potent Bcl-xL PROTAC degrader with an IC50 of 1.3 nM (MOLT-4 cells) and a DC50 of 0.9 nM (Bcl-xL). PZ671 induces apoptosis in MOLT-4 cells. PZ671 effectively inhibits tumor growth and rapidly reverses transient platelet counts reduction in MOLT-4 xenograft mice. PZ671 can be used for the research of cancer, such as small cell lung cancer (SCLC)[1]. (Structure Note: Pink: Bcl-xL ligand (HY-174878); Blue: E3 ligase Ligand (HY-138793); Black: linker; E3-linker (HY-174879))

IC50 & Target[1]

Bcl-xL

 

In Vitro

PZ671 (Compound 5b) (0.4-100 nM, 1-16 h) induces Bcl-xL degradation in MOLT-4 cells[1].

PZ671 (10, 100 nM) degrades Bcl-xL depending on proteasome in MOLT-4 cells[1].

PZ671 (0.4-100 nM, 48 h) induces apoptosis in MOLT-4 cells[1].

PZ671 (30-1000 nM, 48 h) degrades Bcl-xL at concentrations above 1 μM in human platelets[1].

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

PZ671 Related Antibodies

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.4, 1, 3, 11, 33. and 100 nM
Incubation Time: 16 h, and 100 nM for 1, 2, 3, 4, 5, 6 h
Result: Induced dose-dependent Bcl-xL degradation in MOLT-4 cells.
Significantly reduced Bcl-xL levels within 2 h, and almost complete degradation of Bcl-xL after 4 h at 100 nM.

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 10 and 100 nM, pretreatingt with 1 μM MG-132 (HY-13259) for 2 h
Incubation Time: /
Result: Degradation was blocked by proteasome inhibitor MG-132 (HY-13259).

Western Blot Analysis[1]

Cell Line: MOLT-4 cells
Concentration: 0.4, 1, 3, 11, 33. and 100 nM
Incubation Time: 16 h
Result: Dose-dependently increased poly (ADP-ribose) polymerase (PARP) and caspase-3 cleavage.
Significantly reduced β-actin levels with increasing concentrations.

Western Blot Analysis[1]

Cell Line: Human platelets
Concentration: 30, 100, 300 and 1000 nM
Incubation Time: 48 h
Result: Degraded Bcl-xL at concentrations above 1 μM.
In Vivo

PZ671 (1.5 mg/kg/, i.p., q4d for 22 days) markedly suppresses the tumor growth but induces only a transient drop in platelet counts following its administration with rapid recovery from thesecond day onwards in MOLT-4 xenograft mice[1].

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

Animal Model: MOLT-4 xenograft mice (CB-17 SCID, Female, 5-6 weeks)[1]
Dosage: 1.5 mg/kg
Administration: Intraperitoneal injection, every 4 days for 22 days
Result: Markedly suppressed the tumor growth.
Caused a transient ∼72% reduction in platelet counts after a single dose, with rapid recovery from the second day onward.
Molecular Weight

1335.02

Formula

C66H79ClF3N7O11S3
SMILES

O=C(NS(=O)(C1=CC=C(N[C@@H](CSC2=CC=CC=C2)CCN(C)CCOCCOCCOCCCC3=CC4=C(C(N(C(CC5)C(NC5=O)=O)C4)=O)C=C3)C(S(=O)(C(F)(F)F)=O)=C1)=O)C6=CC=C(N7CCN(CC8=C(C9=CC=C(Cl)C=C9)CCC(C)(C)C8)CC7)C=C6
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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PZ671 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:

PZ671PZ 671PZ-671PROTACsBcl-2 FamilyApoptosisBcl-xLSmall cell lung cancerMOLT-4 cellsMOLT-4 xenograft miceInhibitorinhibitorinhibit

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