KB-0118
KB-0118 (BBC0115) is an orally active BET bromodomain inhibitor. KB-0118 selective binds to BRD2 and BRD4 over BRD3, with Kd values of 36.7 μM for BRD2 BD1 and 47.4 μM for BRD4 BD1. KB-0118 inhibits pro-inflammatory cytokines, including TNF, IL-1β, and IL-23a and selectively suppresses Th17 cell differentiation. KB-0118 modulates Th17-driven inflammation occurs through epigenetic suppression of BRD4, confirmed by downregulation of STAT3 and BRD4 target genes. KB-0118 has immunomodulatory effects in inflammatory bowel disease (IBD) model.
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- CAS No.: 2648377-08-4
- 화학식: C17H11NO5
- 분자량:309.27
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
BRD2 BD1 36.7 μM (Kd) |
BRD2 BD2 74.3 μM (Kd) |
BRD4 BD1 47.4 μM (Kd) |
BRD4 BD2 41.7 μM (Kd) |
STAT3 |
IL-1β |
IL-23a |
In Vitro
KB-0118 (1-10 μM, 12 h) downregulates pro-inflammatory cytokines (eg: TNF, MIF, and CSF2) in PMA (HY-18739)/Lonomycin (HY-122466) treated Jurkat cells[1].
KB-0118 (1-10 μM, 12 h) downregulates pro-inflammatory cytokines (eg: IL-1β, IL-6, IL-23a, and Cxcl11) in LPS (HY-D1056) treated RAW 264.7 cells[1].
KB-0118 (5 μM, 5 days) inhibits anti-CD3 and anti-CD28 activated mouse CD4+ T cells proliferation, as evidenced by decreased division, proliferation, expansion, and replication indices[1].
KB-0118 (5 μM, 5 days) reduces the proportion of Th17 cells (RORγt+ IL-17A+), indicating inhibition of Th17 differentiation[1].
KB-0118 (5 μM, 5 days) increases the proportion of Th2 cells (GATA-3+ IL-4+), suggesting it promotes Th2 polarization[1].
KB-0118 (0.01-1 μM, 24 h) increases cell viability in DSS (5 %, 48 h)-treated Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat cells
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Concentration:1 μM, 5 μM, 10 μM
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Incubation Time:Pretreated for 6 h and then co-incubated with PMA/Lonomycin for 6 h
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Result:Downregulated pro-inflammatory cytokines, particularly TNF, MIF, and CSF2, TGFB1, and these reductions were statistically significant at 5 μM and 10 μM.
Upregulated IL-3, IL-4, and IL-26.
In Vivo
KB-0118 (50 mg/kg, p.o., daily for 6 weeks) alleviates T cell-mediated colitis by reducing IL-17a-driven inflammation in a chronic T cell-mediated mice colitis model[1].
KB-0118 (50-250 mg/kg, p.o., for 14 days) shows tolerability in male and female C57BL/6 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS (HY-116282C) (3 % in drinking water)-induced colitis model in male C57BL/6 mice[1].
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Dosage:200 mg/kg
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Administration:In drinking water, for 7days
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Result:Had a significant protective effect on colon length, preserving colon integrity and reducing inflammation compared to the DSS-only group.
Reduced epithelial damage and immune cell infiltration compared to DSS-only mice.
Provided a slight, non-significant reduction in weight loss and the Disease Activity Index (DAI) compared to DSS-only mice.
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Animal Model:A chronic colitis model induced by adoptive transfer of CD45RBhigh T cells into RAG1 KO mice[1].
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Dosage:50 mg/kg
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Administration:Oral gavage (p.o.), daily for 6 weeks
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Result:Attenuated weight loss and increased colon length compared to vehicle-treated controls.
Reduced epithelial damage and immune cell infiltration in the colon, showing greater efficacy than MS402 (HY-120000).
Reduced IL-17a levels in the DSS-treated colons.
Down-regulated critical genes for T cell activation and cytotoxicity, such as Cd3e, Lck, and Stat4, as well as integrin genes like Itgam and Itgal (bulk RNA sequencing).
Reduced expression of genes regulated by immune-related TFs, such as IRF8, FOXO1, and RUNX1 (bulk RNA sequencing).
Chemical Information
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CAS No. 2648377-08-4
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분자량 309.27
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화학식 C17H11NO5
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SMILES
O=C1C(O)=C(C2=CC3=C(C=CN3)C=C2)OC4=C1C(O)=CC(O)=C4
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Synonyms
BBC0115
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KB-0118 Related Classifications
HY-176535 Related Classifications
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