2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation Apoptosis
  3. HDAC NO Synthase TNF Receptor Interleukin Related
  4. HDAC6-IN-80

HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy.

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

HDAC6-IN-80

HDAC6-IN-80 Chemical Structure

CAS No. : 3118852-74-4

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HDAC6-IN-80 Related Antibodies

Top Publications Citing Use of Products

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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nNOS iNOS eNOS

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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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

HDAC6-IN-80 is an orally active, selective HDAC6 inhibitor with an IC50 of 8.5 nM. HDAC6-IN-80 inhibits lipopolysaccharide-induced microglial activation, reduces the levels of iNOS, COX-2, TNF-α and IL-6, and alleviates sensory hypersensitivity behaviors. HDAC6-IN-80 can be used for the research of inflammatory pain and chemotherapy-induced peripheral neuropathy[1].

IC50 & Target[1]

HDAC6

8.5 nM (IC50)

IL-6

 

iNOS

 

In Vitro

HDAC6-IN-80 (Compound 36) (1-10 μg/mL; 6.5-24.5 h) inhibits LPS-induced inflammatory responses in BV2 microglial cells by reducing nitrite levels and the mRNA and protein expression of proinflammatory mediators (iNOS, COX-2, TNF-α, IL-6), and does not affect cell viability at concentrations up to 10 μg/mL[1].

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

HDAC6-IN-80 Related Antibodies
Parmacokinetics
Species Dose Route Cmax T1/2 Tmax AUC0-t AUC0-∞ Bioavailability CL
Mice[1] 3 mg/kg i.v. / 0.15 h / 106 ng·h/mL 106 ng·h/mL / 478 mL/min/kg
Mice[1] 10 mg/kg p.o. 111 ng/mL 0.50 h 0.25 h 78.6 ng·h/mL 80.9 ng·h/mL 22.85 % /
In Vivo

HDAC6-IN-80 (Compound 36) (15-60 mg/kg; p.o.; single administration) dose-dependently alleviates carrageenan (HY-125474)-induced inflammatory pain in mice, with an ED50 of 35.66 mg/kg[1].
HDAC6-IN-80 (15-60 mg/kg; p.o.; single administration) dose-dependently alleviates Paclitaxel (HY-B0015)-induced neuropathic pain in mice, with an ED50 of 37.89 mg/kg[1].
HDAC6-IN-80 (15-60 mg/kg; p.o.; single administration) exerts only extremely weak effects on motor coordination in mice at doses up to 30 mg/kg, and causes significant impairment only at the 60 mg/kg dose[1].

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

Animal Model: ICR (male, 20-32 g)[1]
Dosage: 15 mg/kg; 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
Result: Produced a maximum possible effect (MPE) of 45.84% at 30 mg/kg.
Dose-dependently increased mechanical paw withdrawal thresholds (MWTs) across all tested doses.
Significantly elevated the area under the curve (AUC) of MWTs in a dose-related manner.
Achieved an ED50 value of 35.66 mg/kg for alleviating carrageenan-induced allodynia.
Animal Model: ICR (male, 20-32 g)[1]
Dosage: 15 mg/kg; 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
Result: Dose-dependently increased mechanical withdrawal thresholds (MWTs) in paclitaxel-treated mice.
Achieved an ED50 value of 37.89 mg/kg for alleviating paclitaxel-induced mechanical allodynia.
Significantly elevated the area under the curve (AUC) of MWTs in a dose-related manner.
Animal Model: ICR (male, 20-32 g)[1]
Dosage: 15 mg/kg; 30 mg/kg; 60 mg/kg
Administration: p.o.; single dose
Result: Did not induce statistically significant motor impairment at 15 and 30 mg/kg.
Significantly reduced rotarod latency at 30, 60, and 90 minutes post-administration at 60 mg/kg (p < 0.01 vs vehicle).
Molecular Weight

381.43

Formula

C21H23N3O4
CAS No.
SMILES

ONC(CCCCCOC1=CC=C(C2=NC(C3=CC=C(C)C=C3)=NO2)C=C1)=O
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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HDAC6-IN-80 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:

HDAC6-IN-803118852-74-4HDACNO SynthaseTNF ReceptorInterleukin RelatedHistone deacetylasesNitric oxide synthasesNOSTumor Necrosis Factor ReceptorTNFRILIL-6BV2 microglial cellsCOX-2iNOSchemotherapy-induced peripheral neuropathyinflammatory painHDAC6microgliamiceTNF-αInhibitorinhibitorinhibit

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