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Chemical Structure| 71-00-1 Chemical Structure| 71-00-1
Chemical Structure| 71-00-1

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CAS No.: 71-00-1

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L-Hisidine is mitochondrial glutamine transport inhibitor, can be used in the biosynthesis of proteins.

Synonyms: Glyoxaline-5-Alanine; NSC 137773; Histidine

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Yangfeng Li ; Zhengnan Shen ; Kiira Ratia ; Jiong Zhao ; Fei Huang ; Oleksii Dubrovyskyii , et al.

Abstract: The bromodomain and extra-terminal domain (BET) proteins are epigenetic readers, regulating transcription via two highly homologous tandem bromodomains, BD1 and BD2. Clinical development of nonselective pan-BD BET inhibitors has been challenging, partly due to dose-limiting side effects such as thrombocytopenia. This has prompted the push for domain-selective BET inhibitors to achieve a more favorable therapeutic window. We report a structure-guided drug design campaign that led to the development of a potent BD1-selective BET inhibitor, 33 (XL-126), with a Kd of 8.9 nM and 185-fold BD1/BD2 selectivity. The high selectivity was first assayed by SPR, validated by a secondary time-resolved fluorescence energy transfer assay, and further corroborated by BROMOscan (~57–373 fold selectivity). The cocrystal of 33 with BRD4 BD1 and BD2 demonstrates the source of selectivity: repulsion with His437 and lost binding with the clamp. Notably, the BD1 selectivity of BET inhibitor 33 leads to both the preservation of platelets and potent anti-inflammatory efficacy.

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Product Details of H-His-OH

CAS No. :71-00-1
Formula : C6H9N3O2
M.W : 155.15
SMILES Code : N[C@@H](CC1=CNC=N1)C(O)=O
Synonyms :
Glyoxaline-5-Alanine; NSC 137773; Histidine
MDL No. :MFCD00064315

Safety of H-His-OH

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338
 

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