2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. KTT-1

KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases.

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KTT-1

KTT-1 Chemical Structure

CAS No. : 2397562-26-2

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KTT-1 Related Antibodies

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

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Description

KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases[1][2].

IC50 & Target[1][2]

HDAC2

 

In Vitro

KTT-1 (25-200 nM; Bone Marrow-Derived Macrophages (BM cells)) reduces the number of osteoclasts and the expression of key osteoclast differentiation genes[1].
KTT-1 (25-100 nM; Bone Marrow-Derived Macrophages (BMDMs)) reduces IL-1β and IL-6 production without affecting TNF-α production[1].
KTT-1 (Day 6, Day 8, Day 10; Bone Marrow-Derived Macrophages (BM cells)) alters gene expression and arrests osteoclast differentiation[1].

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

KTT-1 Related Antibodies
In Vivo

KTT-1 (0.03 mg/mL (6 mg/kg/day); drinking water; 10 consecutive days) attenuates arthritis severity in CIA model[1].
KTT-1 (0.03 mg/mL (6 mg/kg/day); drinking water; 22 days) alleviates arthritis severity in CAIA model[1].

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

Animal Model: DBA/1JJmsSlc (male, 6-7 weeks old, collagen-induced arthritis (CIA) model)[1]
Dosage: 0.03 mg/mL (6 mg/kg/day)
Administration: Drinking water; 10 consecutive days
Result: Arthritis severity was significantly attenuated, as evidenced by reduced clinical scores and histological scores.
Showed markedly reduced synovial inflammation and immune cell infiltration, with preservation of normal joint architecture.
Animal Model: DBA/1JJmsSlc (male, 6-7 weeks old, collagen antibody-induced arthritis (CAIA) model)[1]
Dosage: 0.03 mg/mL (6 mg/kg/day)
Administration: Drinking water; 22 days
Result: Arthritis severity was significantly alleviated, as indicated by reduced clinical scores and improved body weight gain.
Molecular Weight

499.54

Formula

C26H21N5O4S
CAS No.
SMILES

O=C(NC1=CC(C2=CC=CO2)=CC=C1N)C(C=C3)=CC=C3C(N=N4)=CN4CS(=O)(C5=CC=CC=C5)=O
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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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KTT-1 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:

KTT-12397562-26-2KTT1KTT 1HDACHistone deacetylasesHistone deacetylase 2 inhibitor replica-exchange umbrella sampling moleculer dynamics simulation Osteoclast histone deacetylaseInhibitorinhibitorinhibit

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