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BMS-066

Name: BMS-066
Brand: TargetMol
SKU: T14669
Price: 548 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: BMS066, BMS 066) Copy Product Info

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Synonyms: BMS066, BMS 066

Catalog No. T14669 Copy Product Info

Purity: 99.24%

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BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor with IC50 values of 9 nM and 72 nM, respectively. BMS-066 is used in kinase signaling research systems to investigate NF-κB pathway regulation, JAK/STAT-associated signaling modulation, and inflammatory response control in cellular disease models.

Cas No. 914946-88-6

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Pack Size	Price	USA Stock	Global Stock
1 mg	$548	-	In Stock
5 mg	$1,650	-	In Stock
10 mg	$2,230	-	In Stock
25 mg	$3,330	-	In Stock
50 mg	$4,390	-	In Stock
1 mL x 10 mM (in DMSO)	$1,670	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.24%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor with IC50 values of 9 nM and 72 nM, respectively. BMS-066 is used in kinase signaling research systems to investigate NF-κB pathway regulation, JAK/STAT-associated signaling modulation, and inflammatory response control in cellular disease models.
Targets & IC50	IKKβ:9 nM, TYK2:72 nM
In vitro	BMS-066 demonstrates significant inhibition of IKKβ-catalyzed phosphorylation in vitro, with a potent IC50 of 9 nM, exhibiting over 500-fold selectivity towards IKKβ compared to IKKα. In assays with six kinases that were more than 75% inhibited at 10 μM, BMS-066 displayed over 30-fold selectivity over the next most susceptible kinase (Brk), indicating its specificity. Additionally, BMS-066 showed IC50 values of 72 and 1020 nM in Tyk2 pseudokinase domain probe displacement and IL-23-stimulated reporter assays respectively. A broader selectivity assessment against 155 kinases at 10 μM revealed that only six were inhibited more than 75%, confirming BMS-066's greater than 400-fold selectivity for IKKβ over 95% of the kinases tested. BMS-066 also effectively inhibits LPS-stimulated cytokine production in human peripheral blood mononuclear cells (PBMCs) at both protein and mRNA levels, with similar IC50 values around 200 nM, and it inhibits IKKβ-mediated phosphorylation of IkBα in LPS-stimulated cells with a comparable efficacy.
In vivo	Method: Dose-dependent evaluation of BMS-066 was performed in an experimental arthritis model using histological analysis, bone density measurement, and microcomputed tomography. Result: Low-dose BMS-066 (5 mg/kg) reduced inflammation and produced more focal and less severe bone resorption compared with control. At 10 mg/kg, joints were normal or showed minimal inflammation and bone resorption. Bone density and microCT analysis showed dose-dependent protection against bone loss, pitting, porous bone formation, and bone fusion. Serum exposure indicated approximately 3 h coverage of mouse whole-blood IC50 after a single dose, and IKKβ inhibition reduced TNF-α and IL-1β production in tissues.
Synonyms	BMS066, BMS 066

Chemical Properties

Molecular Weight	379.42
Formula	C₁₉H₂₁N₇O₂
Cas No.	914946-88-6
Smiles	O=C(NCC1=NC(=CC=C1)C=2N=C3NC(NC)=C4N=CN(C4=C3C2)C)COC
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (210.85 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6356 mL	13.1780 mL	26.3560 mL	131.7801 mL
5 mM	0.5271 mL	2.6356 mL	5.2712 mL	26.3560 mL
10 mM	0.2636 mL	1.3178 mL	2.6356 mL	13.1780 mL
20 mM	0.1318 mL	0.6589 mL	1.3178 mL	6.5890 mL
50 mM	0.0527 mL	0.2636 mL	0.5271 mL	2.6356 mL
100 mM	0.0264 mL	0.1318 mL	0.2636 mL	1.3178 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc