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製品番号: HY-184408

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AAP-SO2

AAP-SO2 is a Bactericide and Mycobacterium tuberculosis RNA polymerase (Mtb RNAP) inhibitor, with an IC₅₀ of 0.025 μM against Mtb RNAP. AAP-SO2 allosterically slows the nucleotide addition rate during transcriptional elongation and enhances transcription termination efficiency. AAP-SO2 exhibits increased activity against β^S450L-type Mtb, possesses activity against non-replicating Mtb, and shows whole-cell activity against Mtb and related mycobacterial species. AAP-SO2 reduces the overall emergence rate of Rifampicin (HY-B0272) tolerance in Mtb, alters the mutation spectrum, and decreases the proportion of β^S450L-type Rifampicin-resistant mutants. AAP-SO2 acts synergistically with Rifampicin to kill non-replicating Mtb in a rabbit caseous necrosis model. AAP-SO2 can be used for the research of tuberculosis.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3033990-94-9
分子式: C₂₆H₂₆FN₃O₄S
分子量:495.57

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

AAP-SO2 構造式

CAS 番号: 3033990-94-9

価格（税別）

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	EC₅₀	30 μM Compound: 24	Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 37001025]
A2780	EC₅₀	30 μM Compound: 24	Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 37001025]
HeLa	EC₅₀	30 μM Compound: 24	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 37001025]
HT-29	EC₅₀	30 μM Compound: 24	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 37001025]
MCF7	EC₅₀	30 μM Compound: 24	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 37001025]
NIH3T3	EC₅₀	30 μM Compound: 24	Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Cytotoxicity against mouse NIH3T3 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 37001025]

体外実験

Bacterial InfectionOthers

Bacterial Infection

AAP-SO2 (69 nM; grown to stationary phase) reduces the emergence rate of Rifampicin (HY-B0272) tolerance in wild-type H37Rv Mtb and alters the mutation spectrum to decrease the proportion of βS450L mutations^[1].
AAP-SO2 (7 days) alone eliminates non-replicating Mtb HN878 from rabbit caseous necrosis in vitro, with a casMBC₉₀ of 7.89 µM; it also exerts a synergistic effect with Rifampicin at equimolar concentrations of 0.5 µM and 2 µM^[1].
AAP-SO2 (serial concentrations; 7 days) inhibits the growth of actively replicating wild-type Mtb strains, and the Mtb^βS450L mutant strain is approximately 1.8-fold more sensitive than the wild-type strain^[1].

Others

AAP-SO₂ (10 µM; 10 min) significantly increases the transcription termination efficiency of purified wild-type (WT) and βS450L mutant Mtb RNA polymerase (RNAP) holoenzymes, with a stronger effect on the βS450L mutant^[1].
AAP-SO2 (0.01-10 µM; 5 min) potently inhibits the transcriptional activity of purified wild-type Mtb RNA polymerase holoenzyme, with an IC₅₀ of 0.0251 µM^[1].
AAP-SO2 (10 µM; 10 min) directly binds to purified Mtb RNA polymerase core complex, with a higher binding efficiency than MMV688845^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Genotoxicity/Mutagenicity Study

化学情報

CAS 番号 3033990-94-9
分子量 495.57
分子式 C₂₆H₂₆FN₃O₄S
SMILES

FC1=CC=CC=C1C(N[C@H](CC2=CC=CC=C2)C(NC3=CC=CC=C3N4CCS(CC4)(=O)=O)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Bosch B, et al. Transcription co-inhibition alters drug resistance evolution and enhances Mycobacterium tuberculosis clearance from granulomas. Nature microbiology. 2026 Jan;11(1):180-194. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Minimum order quantity

100 mg

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