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Chemical Structure| 63329-53-3 Chemical Structure| 63329-53-3

Structure of Lobenzarit
CAS No.: 63329-53-3

Chemical Structure| 63329-53-3

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Lobenzar It is an immunomodulator mainly used for treating autoimmune diseases like rheumatoid arthritis. It alleviates inflammation by inhibiting the production of inflammatory mediators and modulating immune cell activity, protecting joint function.

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Product Citations

Product Citations

Shifali Shishodia ; Raymundo Nuñez ; Brayden P. Strohmier ; Karina L. Bursch ; Christopher J. Goetz ; Michael D. Olp , et al.

Abstract: PBRM1 is a subunit of the PBAF chromatin remodeling complex that uniquely contains six bromodomains. PBRM1 can operate as a tumor suppressor or tumor promoter. PBRM1 is a tumor promoter in prostate cancer, contributing to migratory and immunosuppressive phenotypes. Selective chemical probes targeting PBRM1 bromodomains are desired to elucidate the association between aberrant PBRM1 chromatin binding and cancer pathogenesis and the contributions of PBRM1 to immunotherapy. Previous PBRM1 inhibitors unselectively bind SMARCA2 and SMARCA4 bromodomains with nanomolar potency. We used our protein-detected NMR screening pipeline to screen 1968 fragments against the second PBRM1 bromodomain, identifying 17 hits with Kd values from 45 μM to >2 mM. Structure–activity relationship studies on the tightest-binding hit resulted in nanomolar inhibitors with selectivity for PBRM1 over SMARCA2 and SMARCA4. These chemical probes inhibit the association of full-length PBRM1 to acetylated histone peptides and selectively inhibit growth of a PBRM1-dependent prostate cancer cell line.

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Product Details of Lobenzarit

CAS No. :63329-53-3
Formula : C14H10ClNO4
M.W : 291.69
SMILES Code : O=C(O)C1=CC=C(Cl)C=C1NC2=CC=CC=C2C(O)=O
InChI Key :UGDPYGKWIHHBMB-UHFFFAOYSA-N
Pubchem ID :3946

Safety of Lobenzarit

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.14mL

3.43mL

1.71mL

34.28mL

6.86mL

3.43mL

 

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