2. PROTAC Epigenetics Cell Cycle/DNA Damage Apoptosis
  3. PROTACs HDAC Bcl-2 Family Apoptosis
  4. PROTAC HDAC3 degrader-1

PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia.
(Pink: HDAC3 ligand (HY-181768); Blue: VHL ligand (HY-125845); Black: linker).

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

PROTAC HDAC3 degrader-1

PROTAC HDAC3 degrader-1 Chemical Structure

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PROTAC HDAC3 degrader-1 Related Antibodies

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Description

PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia[1]. (Pink: HDAC3 ligand (HY-181768); Blue: VHL ligand (HY-125845); Black: linker).

IC50 & Target[1]

HDAC3

30.73 nM (DC50)

Bcl-xL

 

Mcl-1

 

In Vitro

PROTAC HDAC3 degrader-1 (b22) (20 nM, 200 nM; 12 h) induces HDAC3 degradation in MV4-11 cells, with 24.4% degradation at 20 nM and 81.8% degradation[1].
PROTAC HDAC3 degrader-1 induces HDAC3 degradation in THP-1 AML cells with a DC50 of 143.1 nM[1].
PROTAC HDAC3 degrader-1 (0.5-1000 nM; 24 h) induces concentration-dependent HDAC3 degradation in MV4-11 cells, with a DC50 of 30.73 nM and a maximum degradation efficiency of 82% after 24 h of treatment[1].
PROTAC HDAC3 degrader-1 (200 nM; 0.5-24 h) induces time-dependent HDAC3 degradation in MV4-11 cells, reaching maximum levels within 8 h and sustaining degradation[1].
PROTAC HDAC3 degrader-1 (8-1000 nM; 12 h) exhibits highly selective degradation of HDAC3 over other HDAC isoforms (HDAC1, HDAC2, HDAC4, HDAC6, HDAC11) in MV4-11 cells at concentrations up to 200 nM, with an effect on HDAC8 only seen at ≥1000 nM after 12 h of treatment[1].
PROTAC HDAC3 degrader-1 (48 h) exhibits moderate antiproliferative activity against MV4-11 AML cells with an IC50 of 1.26 μM after 48 h of treatment, and significantly reduced cytotoxicity against Kasumi-1, THP-1, HL-7702, and iBMDMs cells[1].
PROTAC HDAC3 degrader-1 (0.078-2.500 μM; 48 h) synergizes with Venetoclax (HY-15531) to inhibit MV4-11 cell proliferation, with CI values <1 for all tested concentration combinations after 48 h of treatment[1].
PROTAC HDAC3 degrader-1 (300-600 nM; 48 h) synergizes with Venetoclax to promote apoptosis in MV4-11 cells, with apoptosis rates reaching up to 88.90% after 48 h of combined treatment[1].
PROTAC HDAC3 degrader-1 (150-600 nM; 24 h) synergizes with Venetoclax in MV4-11 cells to downregulate anti-apoptotic proteins Mcl-1 and Bcl-xL, enhance DNA damage (increased γH2A.X), and activate caspase3 cleavage after 24 h of combined treatment, while b22 alone has no significant effect on these proteins[1].

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

PROTAC HDAC3 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 acute myeloid leukemia (AML) cells
Concentration: 20 nM; 200 nM
Incubation Time: 12 h
Result: Induced 24.4% HDAC3 degradation at 20 nM.
Induced 81.8% HDAC3 degradation at 200 nM.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5, 1.4, 4.1, 12.3, 37.0, 111.1, 333.3, 1000 nM
Incubation Time: 24 h
Result: Induced concentration-dependent HDAC3 degradation with a DC50 of 30.73 nM and a maximum degradation efficiency (Dmax) of 82%.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 200 nM
Incubation Time: 0.5, 1, 1, 2, 3, 4, 6, 8, 10, 12, 24 h
Result: Reached maximum HDAC3 degradation within 8 h of treatment.
Sustained degradation levels were maintained for at least 24 h.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 8, 40, 200, 1000 nM
Incubation Time: 12 h
Result: Promoted efficient, dose-dependent degradation of HDAC3 specifically.
Showed no significant effects on HDAC1, HDAC2, HDAC4, HDAC6, or HDAC11 at concentrations up to 200 nM.
Caused a significant effect on HDAC8 only at concentrations ≥ 1000 nM.

Cell Proliferation Assay[1]

Cell Line: MV4-11 cells
Concentration: 2.500, 1.250, 0.625, 0.313, 0.156, 0.078 μM (PROTAC HDAC3 degrader-1); 0.031, 0.063, 0.125 μM (Venetoclax)
Incubation Time: 48 h
Result: Produced combination index (CI) values < 1 for all tested combinations with Venetoclax, indicating synergistic antiproliferative effects.
CI values ranged from 0.066 to 0.611 across the tested concentration combinations.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 300, 600 nM (PROTAC HDAC3 degrader-1 alone); 300, 600 nM (PROTAC HDAC3 degrader-1) + 30, 60 nM (Venetoclax) (HY-15531) (combined)
Incubation Time: 48 h
Result: Induced 11.40% apoptosis at 300 nM when used alone.
Induced 14.16% apoptosis at 600 nM when used alone.
Increased apoptosis rate to 63.10% when combined with 30 nM Venetoclax at 300 nM b22.
Increased apoptosis rate to 79.10% when combined with 30 nM Venetoclax at 600 nM.
Increased apoptosis rate to 69.50% when combined with 60 nM Venetoclax at 300 nM.
Increased apoptosis rate to 88.90% when combined with 60 nM Venetoclax at 600 nM.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 150, 300, 600 nM (PROTAC HDAC3 degrader-1 alone); 150, 300, 600 nM (PROTAC HDAC3 degrader-1) + 30, 60 nM (Venetoclax) (combined)
Incubation Time: 24 h
Result: Did not significantly alter Mcl-1 or Bcl-xL protein levels when used alone.
Dose-dependently downregulated Mcl-1 and Bcl-xL when combined with Venetoclax.
Increased γH2A.X levels (a marker of DNA double-strand breaks) when combined with Venetoclax.
Reduced pro-caspase3 levels when combined with Venetoclax.
Synergistically increased cleaved caspase3 levels when combined with Venetoclax.
Parmacokinetics
Species Dose Route Cmax AUC0-inf T1/2 Vss CL
Mice[1] 2 mg/kg i.v. 1454.29 ng/mL 807.25 ng·h/mL 1.81 h 4.27 L/kg 45.64 mL/min/kg
In Vivo

PROTAC HDAC3 degrader-1 (2 mg/kg; i.v.; single dose) results in moderate systemic exposure, a terminal half-life of 1.81 h, and a total plasma clearance of 45.64 mL/min/kg in male ICR mice[1].

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

934.16

Formula

C50H63N9O7S
SMILES

O=C([C@H]1N(C([C@@H](NC(CN2CCN(CCN(CC3=CC=C(C(NNCCC)=O)C=C3)C(C4=CC5=CC=CC=C5O4)=O)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC6=CC=C(C7=C(C)N=CS7)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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PROTAC HDAC3 degrader-1 Related Classifications

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  • 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 HDAC3 degrader-1PROTACsHDACBcl-2 FamilyApoptosisHistone deacetylasesubiquitin-proteasome systemapoptosisKasumi-1 cellsDNA damageTHP-1 AML cellsBcl-xLMV4-11 cellsacute myeloid leukemiaMcl-1HDAC3Inhibitorinhibitorinhibit

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