Deltasonamide 1

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Deltasonamide 1 

Deltasonamide 1 是 PDE6δ-KRas 的抑制剂，其 KD 值为 203 pM。

Deltasonamide 1

Deltasonamide 1 Chemical Structure

CAS No. : 2088485-33-8

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生物活性

Deltasonamide 1 is a PDE6δ-KRas inhibitor, with a KD of 203 pM[1].

体外研究
(In Vitro)

Deltasonamide 1 binds inside the PDE6δ binding pocket, including H-bonds to R61, Q78, E88, and Y149 sidechains, to the carbonyl of C56, two water molecule-mediated H-bonds to the Glu 88 side-chain and the amide proton of M118, two aromatic–p interactions to the indole side-chains of W32 and W90, and one M117-aryl interaction[1].
Deltasonamide 1 migrates slowly but show enhanced apparent permeability from the B to A side suggesting a potential interaction with efflux transporters. Deltasonamides results in a reduced interacting fraction of RheB-PDE6δ[1].
Deltasonamide 1 results in a strongly reduced proliferation, even at submicromolar concentrations in MiaPaCa-2 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: RTCA of hPDAC cell lines.
Concentration: 0.375, 0.75, 1.5, 3, 6, 12 μM.
Incubation Time: 60 h.
Result: Inhibited proliferation of human pancreatic cancer cell lines.

分子量

647.25

Formula

C30H39ClN6O4S2
CAS 号

2088485-33-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Pablo Martín-Gago, et al. A PDE6δ-KRas Inhibitor Chemotype With Up to Seven H-Bonds and Picomolar Affinity That Prevents Efficient Inhibitor Release by Arl2. Angew Chem Int Ed Engl. 2017 Feb 20;56(9):2423-2428.

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