Bay 65-1942 hydrochloride

Name: Bay 65-1942 hydrochloride
Brand: MedChemExpress
SKU: HY-50948
Rating: 5.0 (4 reviews)

Cat. No.: HY-50948 Purity: 99.39%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.

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

Bay 65-1942 hydrochloride Chemical Structure

CAS No. : 600734-06-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 220	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 220	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 113	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 360	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1020	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1600	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Bay 65-1942 hydrochloride:

Bay 65-1942 (R form) In-stock
Bay 65-1942 free base Get quote

3 Publications Citing Use of MCE Bay 65-1942 hydrochloride

RT-PCR

: Bay 65-1942 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2016 Aug 4;35(31):4036-47. [Abstract]; Effect of BEZ235 and Bay 65–1942 on CXCL1, CXCL2 and CXCL8 mRNAs in FUOV1, NIH:OVCAR3 and IGROV1 cells. Quantitative RT-PCR analysis is performed in cells treated with indicated inhibitors or DMSO control for 6 h.

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IKK-α IKK-β IKK IKKε TBK1

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.

IC₅₀ & Target^[1]

IKKβ

In Vitro

Delivery of Bay 65-1942 prior to ischemia significantly decreases left ventricular infarct size compared with animals receiving vehicle. Compared with sham animals, animals receiving vehicle have a significant increase in the infarct-to-area at risk (AAR) ratio (70.7±3.4 vs. 5.8±3.4%, P<0.05). This ratio is significantly reduced by treatment with Bay 65-1942 at each time point (prior to ischemia 42.7±4.1%, at reperfusion 42.7±7.5%, 2 h of reperfusion 29.4±5.2%; each group P<0.05 vs. vehicle). Animals pretreated with Bay 65-1942 (n=3) have significantly attenuated CK-MB levels compared with those animals without treatment prior to IR (14,170 ±3,219 units, P<0.05 vs. vehicle)^[1].

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

In Vivo

Inhibitors of MEK (AZD6244) and IKK (BAY 65-1942) are used at their IC₅₀ concentrations, as determined by a 48 hour MTS assay, which achieve sufficient inhibition of kinase activity. MYL-R cells are treated for 24 hours with AZD6244 (5 μM), BAY 65-1942 (10 μM), or a combination of these inhibitors at the same concentrations. AZD6244 and BAY 65-1942 demonstrate synergistic inhibition of cell viability at the dose combination (5 μM AZD6244+10 μM BAY 65-1942), which correlates with IC₇₅ (CI = 0.48±0.01). Synergism is also indicated at the IC₅₀ (CI = 0.56±0.09) and IC₉₀ (CI = 0.46±0.02) dose combinations reported by the software (CI values are the mean of three independent experiments, ± standard deviation). AZD6244 and BAY 65-1942 treatment induces 2- and 1.3-fold caspase 3/7 activation, respectively, compared to the DMSO-treated cells. Treatment with a combination of AZD6244 plus BAY 65-1942 leads to a 3.2-fold increase in caspase 3/7 activity^[2].

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

Molecular Weight

431.91

Formula

C₂₂H₂₆ClN₃O₄

CAS No.

600734-06-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1OCC2=C([C@H]3CNCCC3)C=C(C4=C(O)C=CC=C4OCC5CC5)N=C2N1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (115.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2.17 mg/mL (5.02 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3153 mL	11.5765 mL	23.1530 mL
5 mM	0.4631 mL	2.3153 mL	4.6306 mL
10 mM	0.2315 mL	1.1576 mL	2.3153 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.39%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (253 KB) RP-HPLC (244 KB)

Handling Instructions (2659 KB)

References

[1]. Inhibition of IκB kinase-β protects dopamine neurons against lipopolysaccharide-induced neurotoxicity By Zhang, Feng; Qian, Li; Flood, Patrick M.; Shi, Jing-Shan; Hong, Jau-Shyong; Gao, Hui-Ming J Pharmacol Exp Ther. 2010 June; 333(3): 822-833. [Content Brief]

[2]. Cooper MJ, et al. Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One. 2013 Jun 24;8(6):e66755. [Content Brief]

Cell Assay ^[2]	Cell viability is determined by seeding MYL-R cells on a 96-well plate at 4×10⁴ cells/well in 100 µL RPMI growth medium supplemented with kinase inhibitors. Growth media and kinase inhibitors are replenished at 24 hours, and at 48 hours. 20 µL of MTS assay reagent is added to each well. The plate is returned to the incubator for approximately 1 hour and the absorbance at 490 nm is recorded. For combination index (CI) experiments, cells are grown and assayed. To determine AZD6244 and BAY 65-1942 (10 µM) dose-effects, cells are treated with a series of three-fold dilutions of each drug singly, or in combination while maintaining a constant ratio of 1:2, respectively. Cell viability results are analyzed to derive CI values. The CI values from three independent experiments are averaged^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] Male C57BL/6 mice, 8-10 wk of age are used. To investigate IKKβ inhibition in myocardial IR injury, mice are subjected to 30 min of cardiac ischemia followed by varying periods of reperfusion. An intraperitoneal injection of Bay 65-1942 (5 mg/kg) at appropriate dosing time points is administered. Nontreatment groups receive a vehicle of 10% cremaphor in water. In treatment groups, Bay 65-1942 is delivered either prior to ischemia, at the time of reperfusion, or 2 h after reperfusion injury. Infarct size is measured 24 h after reperfusion injury in sham, vehicle, and each treatment group. To confirm myocardial injury, serum creatine kinase-muscle-brain fraction (CK-MB) levels are measured 1 h after reperfusion in animals pretreated with Bay 65-1942. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Inhibition of IκB kinase-β protects dopamine neurons against lipopolysaccharide-induced neurotoxicity By Zhang, Feng; Qian, Li; Flood, Patrick M.; Shi, Jing-Shan; Hong, Jau-Shyong; Gao, Hui-Ming J Pharmacol Exp Ther. 2010 June; 333(3): 822-833. [Content Brief] [2]. Cooper MJ, et al. Application of multiplexed kinase inhibitor beads to study kinome adaptations in drug-resistant leukemia. PLoS One. 2013 Jun 24;8(6):e66755. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	2.3153 mL	11.5765 mL	23.1530 mL	57.8824 mL
H₂O / DMSO	5 mM	0.4631 mL	2.3153 mL	4.6306 mL	11.5765 mL
DMSO	10 mM	0.2315 mL	1.1576 mL	2.3153 mL	5.7882 mL
	15 mM	0.1544 mL	0.7718 mL	1.5435 mL	3.8588 mL
	20 mM	0.1158 mL	0.5788 mL	1.1576 mL	2.8941 mL
	25 mM	0.0926 mL	0.4631 mL	0.9261 mL	2.3153 mL
	30 mM	0.0772 mL	0.3859 mL	0.7718 mL	1.9294 mL
	40 mM	0.0579 mL	0.2894 mL	0.5788 mL	1.4471 mL
	50 mM	0.0463 mL	0.2315 mL	0.4631 mL	1.1576 mL
	60 mM	0.0386 mL	0.1929 mL	0.3859 mL	0.9647 mL
	80 mM	0.0289 mL	0.1447 mL	0.2894 mL	0.7235 mL
	100 mM	0.0232 mL	0.1158 mL	0.2315 mL	0.5788 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.