2. Epigenetics Immunology/Inflammation Stem Cell/Wnt JAK/STAT Signaling
  3. Epigenetic Reader Domain Interleukin Related STAT
  4. KB-0118

KB-0118 (BBC0115) is 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[1].

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KB-0118 Chemical Structure

KB-0118 Chemical Structure

CAS No. : 2648377-08-4

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KB-0118 Related Antibodies

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Description

KB-0118 (BBC0115) is 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[1].

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.

KB-0118 Related Antibodies

RT-PCR[1]

Cell Line: Jurkat cells
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: Pretreated for 6 h and then co-incubated with PMA/Lonomycin for 6 h
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 (200 mg/kg in drinking water, for 7days) mitigates colitis in DSS (HY-116282C) (3 % in drinking water)-induced colitis model[1].
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 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.

Animal Model: DSS (HY-116282C) (3 % in drinking water)-induced colitis model in male C57BL/6 mice[1].
Dosage: 200 mg/kg
Administration: In drinking water, for 7days
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.
Animal Model: A chronic colitis model induced by adoptive transfer of CD45RBhigh T cells into RAG1 KO mice[1].
Dosage: 50 mg/kg
Administration: Oral gavage (p.o.), daily for 6 weeks
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).
Molecular Weight

309.27

Synonyms

BBC0115

Formula

C17H11NO5
CAS No.
SMILES

O=C1C(O)=C(C2=CC3=C(C=CN3)C=C2)OC4=C1C(O)=CC(O)=C4
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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KB-0118 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:

KB-01182648377-08-4BBC0115KB0118KB 0118BBC 0115BBC-0115Epigenetic Reader DomainInterleukin RelatedSTATILInflammatory bowel diseaseIBDTh 17 cellBRD4DSScolitisJurkatRAW 264.7Inhibitorinhibitorinhibit

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