1. Apoptosis
  2. Bcl-2 Family
  3. Pyridoclax

Pyridoclax (Synonyms: MR-29072)

Cat. No.: HY-12527 Purity: 99.74%
Handling Instructions

Pyridoclax is a potential Mcl-1 inhibitor.

For research use only. We do not sell to patients.

Pyridoclax Chemical Structure

Pyridoclax Chemical Structure

CAS No. : 1651890-44-6

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Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 88 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 137 In-stock
Estimated Time of Arrival: December 31
50 mg USD 478 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Pyridoclax is a potential Mcl-1 inhibitor.

IC50 & Target

Mcl-1

 

In Vitro

Pyridoclax directly binds to Mcl-1. Without cytotoxic activity when administered as a single agent, Pyridoclax induces apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, and mesothelioma cancer cells[1]. Pyridoclax directly binds to Mcl-1, and hence sensitizes ovarian carcinoma cells to Bcl-xL-targeting strategies. Pyridoclax induces apoptosis in ovarian, and also in lung, and mesothelioma cancer cells when it is administrated in combination with Bcl-xL-targeting siRNA or Bcl-xL targeting molecules such as ABT-737 or its orally available derivative ABT-263[2].

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

Molecular Weight

426.51

Formula

C₂₉H₂₂N₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (46.89 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3446 mL 11.7231 mL 23.4461 mL
5 mM 0.4689 mL 2.3446 mL 4.6892 mL
10 mM 0.2345 mL 1.1723 mL 2.3446 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

For donor saturating assays, Hela cells are seeded on 12-well plates and transfected with 200 ng/well of plasmid pRluc-BimL coding for BRET donor and an increasing quantity of BRET acceptor plasmids peYFP-Mcl-1 (or with pCMV-Mcl-1 as a control). Twenty-four hours after transfection, cells are trypsinized, reseeded into white flat bottom 96-well plates, and incubated for another day before measurements. A single donor/acceptor ratio (200/800) is used to carry out the drug treatment assay. After reseeding, cells are then subject to a 16 h Pyridoclax treatment. Light emission at 485 and 530 nm is measured consecutively using the Mithras fluorescence-luminescence detector LB 940 after adding the luciferase substrate, coelenterazine H, at a final concentration of 5 μM. BRET ratios are calculated[1].

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

References
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Pyridoclax
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