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B3063

Sigma-Aldrich

BI-78D3

≥98% (HPLC)

Sinónimos:

4-(2,3-Dihydrobenzol[b][1,4]dioxin-6-yl)-5-(5-nitrothiazol-2-ylthio)-4H-1,2,4-triazol-3-ol

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About This Item

Fórmula empírica (notación de Hill):
C13H9N5O5S2
Número de CAS:
883065-90-5
Peso molecular:
379.37
MDL number:
MFCD12912396
UNSPSC Code:
12352200
PubChem Substance ID:
329773213

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

tan

solubility

DMSO: >10 mg/mL

storage temp.

−20°C

SMILES string

Oc1nnc(Sc2ncc(s2)[N+]([O-])=O)n1-c3ccc4OCCOc4c3

InChI

1S/C13H9N5O5S2/c19-11-15-16-12(25-13-14-6-10(24-13)18(20)21)17(11)7-1-2-8-9(5-7)23-4-3-22-8/h1-2,5-6H,3-4H2,(H,15,19)

InChI key

QFRLDZGQEZCCJZ-UHFFFAOYSA-N

Biochem/physiol Actions

BI-78D3 is a substrate competitive inhibitor of JNK. JNK′s binds to JNK-interacting protein-1 (JIP1) (scaffolding protein) through high affinity D-domain on JIP1. This interaction is needed to place JNK next to target protein. BI-78D3 is a mimetic of a critical peptide structure of JIP1 which binds to JNK away from ATP binding domain preventing JIP1 JNK interaction thus acting as a substrate competitive inhibitor both in vitro and in vivo. The compound represents a growing number of modern kinase inhibitors acting at protein protein interacting areas (scaffolding) rather than ATP binding pockets.

Storage Class

13 - Non Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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JCI insight, 5 (2019-03-13)
AXL overexpression is a common resistance mechanism to anti-cancer therapies, including the resistance to BYL719 (Alpelisib) - the p110α isoform specific inhibitor of phosphoinositide 3-kinase (PI3K) - in esophagus and head and neck squamous cell carcinoma (ESCC, HNSCC respectively). However
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Experimental and therapeutic medicine, 14(6), 5445-5451 (2017-12-30)
Paeoniflorin (PAE), a principal bioactive component of
Yi Li et al.
Biomolecules & therapeutics, 26(5), 458-463 (2017-11-14)
The phosphorylation of JNK is known to induce insulin resistance in insulin target tissues. The inhibition of JNK-JIP1 interaction, which interferes JNK phosphorylation, becomes a potential target for drug development of type 2 diabetes. To discover the inhibitors of JNK-JIP1
Lu Wang et al.
Molecular and cellular endocrinology, 518, 110991-110991 (2020-08-26)
The function of the gonadotropin-releasing hormone (GnRH) neuron is critical to maintain reproductive function and a significant decrease in GnRH can lead to disorders affecting fertility, including hypogonadotropic hypogonadism. Spexin (SPX) is a novel hypothalamic neuropeptide that exerts inhibitory effects
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The limited number of human hematopoietic stem cells (HSCs) has restrained their widespread clinical application. Despite great efforts in recent years, the in vitro expansion of HSCs remains a challenge due to incomplete understanding of the signaling networks underlying HSC
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