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5.31552

Argonaute-2 Inhibitor, BCI-137

Synonym(s):

Argonaute-2 Inhibitor, BCI-137, 2-(2,3-Dioxo-1,2,3,4-tetrahydroquinoxaline-6-sulfonamido) propanoic acid, N-((2,3-Dihydroxy-6-quinoxalinyl)sulfonyl)alanine, Ago2 Inhibitor, BCI137

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Size/SKUAvailabilityPrice
25 mg
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$292.00

About This Item

Empirical Formula (Hill Notation):
C11H11N3O6S
CAS Number:
112170-24-8
Molecular Weight:
313.29
MDL number:
MFCD05148320
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
3157172
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light

$292.00

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assay

≥97% (HPLC)

Quality Segment

100

form

solid

potency

126 μM Kd

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

gray-white

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

SMILES string

CC(C(=O)O)NS(=O)(=O)C1=CC2=C(C=C1)NC(=O)C(=O)N2

General description

A cell-permeable dioxotetrahydroquinoxaline compound that mimics uridine monophosphate for affinity interaction at the Argonaute-2 (Ago2) Mid domain (KD = 126 µM) and effectively inhibits Ago2 cellular miRNA loading in acute promyelocytic leukemia (APL) NB4 cultures (% inhibition by RIP = 79%/miR-107, 73%/let-7a, 73%/miR-223, 68%/miR-26a, 53%/miR-60a; 100 nM for 48 h) without affecting cellular Ago2 stability. Consistent with the involvement of Ago2 in heterochromatic miR-155HG silencing, BCI-137 is reported to decrease miR-155HG promoter region-associated Ago2 with a concomitant acetylation induction of the promoter region-associated histone H4 (70% reduced Ago2 association and 300% enhanced H4 acetylation, respectively, by ChIP; 10 µM). Likewise, Ago2 inhibition by BCI-137 is shown to boost Retinoic Acid-(RA, Cat. no. 554720) induced NB4 granulocyte differentiation as a result of greatly upregulated expression of the differentiation-related miRNAs (140% and 255% increased miR-26a and miR-223 level, respectively, compared to 100 nM RA stimulation alone for 96 h) without affecting NB4 proliferation or viability (up to 10 µM and 96 h with or without 100 nM RA stimulation).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Argonaute-2
Reversible: yes

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Masciarelli, S., et al. 2014. ACS Chem. Biol.9, 1674.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Argonaute-2 Inhibitor, BCI-137

Sigma-Aldrich

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Sigma-Aldrich

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Sigma-Aldrich

317496

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Sigma-Aldrich

566324

SIRT2 Inhibitor, AGK2

description

-

description

The Bcl-2 Inhibitor II, YC137, also referenced under CAS 810659-53-1, controls the biological activity of Bcl-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

description

The Dual Specificity Protein Phosphatase 1/6 Inhibitor, BCI controls the biological activity of Dual Specificity Protein Phosphatase 1/6. Primarily used for Phosphorylation & Dephosphorylation apps.

description

The SIRT2 Inhibitor, AGK2, also referenced under CAS 304896-28-4, controls the biological activity of SIRT2. This small molecule/inhibitor is primarily used for Cell Structure applications.

assay

≥97% (HPLC)

assay

≥90% (HPLC)

assay

≥95% (HPLC)

assay

≥95% (HPLC)

form

solid

form

solid

form

solid

form

solid

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 100 mg/mL

solubility

DMSO: 5 mg/mL, ethanol: 5 mg/mL

solubility

DMSO: 50 mg/mL

solubility

DMSO: 2.5 mg/mL

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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