2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation Apoptosis
  3. HDAC NOD-like Receptor (NLR) Caspase Interleukin Related
  4. HDAC3 degrader-2

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.

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HDAC3 degrader-2

HDAC3 degrader-2 Chemical Structure

CAS No. : 3110847-73-6

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HDAC3 degrader-2 Related Antibodies

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NLRP3 NLRP1 NOD1 NOD2

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis[1].

In Vitro

HDAC3 degrader-2 (compound GS-1) (25-50 μM; 24 h) exhibits only extremely low cytotoxicity in HEK293 and L02 cells. After 24 h of treatment, the relative cell viability remains above 50% at both 25 μM and 50 μM concentrations[1].
HDAC3 degrader-2 (0-10 μM; 2-24 h) potently and selectively degrades HDAC3 in THP-1 cells, with a DC50 of 1.24 μM after 24 h of treatment, while exerting minimal effects on the levels of HDAC1 and HDAC2[1].
HDAC3 degrader-2 (5-20 μM; 24 h) inhibits the activation of NLRP3 inflammasome in THP-1-derived macrophages via selective degradation of HDAC3, reduces the levels of mature IL-1β and caspase-1, and suppresses ASC speck formation without altering the expression of inflammasome components[1].

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

HDAC3 degrader-2 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: L02, HEK293
Concentration: 25 μM, 50 μM
Incubation Time: 24 h
Result: Resulted in 94.29±1.07% relative cell viability in HEK293 cells and 86.65±3.54% relative cell viability in L02 cells at 25 μM.
Resulted in 69.98±3.37% relative cell viability in HEK293 cells and 77.45±3.06% relative cell viability in L02 cells at 50 μM.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ F
Rat[1] 5 mg/kg i.v. 2.82 h 0.0833 h 9473 ng/mL 3094 ng·h/mL 3133 μg·h/mL 0.354 h 0.513 h /
Rat[1] 15 mg/kg i.p. 4.55 h 6.67 h 1222 ng/mL 15322 ng·h/mL 15772 ng·h/mL 7.23 h 7.95 h 67.2 %
In Vivo

HDAC3 degrader-2 (15 mg/kg; intraperitoneal injection; single administration) exerts potent protective effects against LPS (HY-D1056)-induced endotoxic shock in male C57BL/6 mice[1].
HDAC3 degrader-2 (15 mg/kg; i.p.; daily; for 11 consecutive days) significantly ameliorates DSS (HY-116282C)-induced colitis in male C57BL/6 mice[1].
HDAC3 degrader-2 (7.5-15 mg/kg; i.p.; two administrations) exerts dose-dependent efficacy against acute gouty arthritis induced by Uric acid sodium (MSU) (HY-B2130A) in male C57BL/6 mice[1].

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

Animal Model: C57BL/6 (male) treated LPS[1]
Dosage: 15 mg/kg
Administration: i.p.; single dose
Result: Achieved 80% survival at 84 hours.
Achieved 70% survival at 120 hours.
Animal Model: C57BL/6 (male) treated DSS[1]
Dosage: 15 mg/kg
Administration: i.p.; daily; 11 consecutive days
Result: Restored colon length.
Significantly attenuated weight loss.
Reduced the disease activity index (DAI) score.
Improved mucosal integrity.
Reduced epithelial damage.
Partially restored crypt architecture and goblet cell abundance.
Degraded HDAC3 protein in colon tissues.
Suppressed the expression of activated caspase-1 and IL-1β.
Animal Model: C57BL/6 (male) treated MSU[1]
Dosage: 7.5-15 mg/kg
Administration: i.p.; two doses (1 hour pre-MSU injection and 12 hours post-MSU injection)
Result: Suppressed joint swelling.
Maintained 100% survival in mice treated with 15 mg/kg dose without observable adverse effects.
Resulted in minimal inflammatory infiltration, no crystal deposition, and no tissue damage in treated joints.
Molecular Weight

883.17

Formula

C54H70N6O5
CAS No.
SMILES

C[C@]12[C@]3(C([C@@]4([H])[C@@](CC3)(CC[C@@](C)(C4)C(N5CCN(C6=CC=C(C=C6)NC(CCCCCC(NC7=C(C=CC=C7)N)=O)=O)CC5)=O)C)=CC([C@]1([H])[C@@]8([C@@](C(C)(C(C(C#N)=C8)=O)C)([H])CC2)C)=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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HDAC3 degrader-2 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:

HDAC3 degrader-23110847-73-6HDACNOD-like Receptor (NLR)CaspaseInterleukin RelatedHistone deacetylasesILTHP-1 cellscaspase-1THP-1-derived macrophagesNLRP3 inflammasomeIL-1βHDAC3L02C57BL/6 male miceHEK293Lys367Inhibitorinhibitorinhibit

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