1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. 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 Chemische Struktur

CAS. Nr. : 2397562-26-2

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Beschreibung

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.

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.
Molekulargewicht

499.54

Formel

C26H21N5O4S

CAS. Nr.
SMILES

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

Versand

Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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