2. NF-κB Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  3. IKK JAK
  4. BMS-066

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.

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

BMS-066 Chemical Structure

BMS-066 Chemical Structure

CAS No. : 914946-88-6

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Based on 1 publication(s) in Google Scholar

BMS-066 Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.

IC50 & Target[1][2]

IKKβ

9 nM (IC50)

Tyk2

72 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
PBMC IC50
150 nM
Compound: 4m, BMS-066
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 4 hrs by ELISA
Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release treated for 5 mins before LPS challenge measured after 4 hrs by ELISA
[PMID: 22018461]
In Vitro

BMS-066 is shown to inhibit IKKβ-catalyzed phosphorylation of IKKβ in vitro with an IC50 of 9 nM and is more than 500-fold selective for IKKβ over the closely related IKKα. To understand the selectivity on a more comprehensive scale, BMS-066 is assayed against 155 additional kinases at 10 μM, and only six of these kinases are inhibited more than 75%. This indicates that BMS-066 is more than 400-fold selective for IKKβ over more than 95% of the kinases tested. For the six kinases showing more than 75% inhibition at 10 μM, IC50 values are determined in dose-response assays and BMS-066 is shown to be more than 30-fold selective against even the next most potently inhibits kinase (Brk). BMS-066 inhibits LPS-stimulated cytokine production in human peripheral blood mononuclear cells, both at the protein and message level, with IC50 values of approximately 200 nM against these endpoints. BMS-066 inhibits the IKKβ-catalyzed phosphorylation of IkBα in LPS stimulated cells with a similar IC50 value[1]. BMS-066 shows IC50 values of 72 and 1020 nM against the Tyk2 pseudokinase domain probe displacement and IL-23-stimulated reporter assays, respectively[2].

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

BMS-066 Related Antibodies
In Vivo

Once daily oral doses of 5 and 10 mg/kg starting at the time of adjuvant injection on day 1 significantly reduces paw swelling compared with vehicle-treated rats at the end of the study, with the high dose showing nearly complete suppression. The talocrural (ankle) joint space is narrowed. Inflammatory exudates containing neutrophils and cell debris are also evident within the joint space. The joints from animals receiving 10 mg/kg BMS-066 are normal or show minimal changes in both inflammation and bone resorption. Clear reduction of inflammation is also evident in the low dose of BMS-066 (5 mg/kg) and the bone resorption seems to be more focal and less severe compared with the control. Microcomputed tomography of the hind limbs also show that BMS-066 provides a dose-dependent protection against the pitting, loss of bone mass, woven porous bone, and fusion of the small bones evident in the rats. Bone density measurements also show a clear dose-dependent benefit of treatment with BMS-066. Serum drug level measurements in satellite animals on the first day of dosing show that a single dose provides coverage for approximately 3 h (6 h daily with twice daily dosing) of the mouse whole-blood IC50 value against LPS-induced TNF-α. It is also showed that IKKβ inhibitors suppress TNF-α and IL-1β production within these tissues in experimental arthritis model[1].

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

379.42

Formula

C19H21N7O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN1C=NC2=C1C(C=C(C3=CC=CC(CNC(COC)=O)=N3)N4)=C4N=C2NC
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 : 100 mg/mL (263.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6356 mL 13.1780 mL 26.3560 mL
5 mM 0.5271 mL 2.6356 mL 5.2712 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (6.59 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.59 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:

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(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:
%
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% 
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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).
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
References
Cell Assay
[1]

When measuring the inhibition by BMS-066 of the phosphorylation of IkBα in human PBMCs, cells at a density of 1×107 per mL in RPMI 1640 medium supplemented with 10% FBS are preincubated for 30 min BMS-066 at 37°C. Cells are then stimulated for 5 min with LPS (100 ng/mL) and pelleted by rapid centrifugation; the pellets are solubilized by use of ice-cold 10×cell lysis buffer. To measure effects on transcription, human PBMCs are plated on 24-well plates at a density of 3×106 cells/well in RPMI 1640 medium plus 10% FBS and HEPES with varying concentrations of BMS-066 (0-10 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats, Mice[1]
Male Lewis rats (225 g) are used. Vehicle (0.02 N HCl) or BMS-066 in vehicle is administered by oral gavage beginning on the day of adjuvant challenge. Eight animals are included in each treatment group. Male Lewis rats (250 g) are immunized intraperitoneally with 200 μg/rat of keyhole limpet hemocyanin diluted in phosphate-buffered saline. BMS-066 in 0.02 N HCl is administered by oral gavage once daily beginning on the day of immunization. Blood samples were collected on day 7 and on day 14 under isoflurane anesthesia. Male DBA/1 mice (20-25 g) are immunized with 200 μg/mouse of bovine type II collagen in 0.1 mL at the base of the tail on day 0 and on day 21. Vehicle (0.02 N HCl) or BMS-066 in vehicle is administered by oral gavage twice daily beginning on day 21. Mice were monitored after the second immunization for the development of paw inflammation. Each paw was individually scored as follows: 0, normal; 1, one or more swollen digits; 2, mild paw swelling; 3, moderate paw swelling; 4, fusion of joints/ankylosis[1].

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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6356 mL 13.1780 mL 26.3560 mL 65.8900 mL
5 mM 0.5271 mL 2.6356 mL 5.2712 mL 13.1780 mL
10 mM 0.2636 mL 1.3178 mL 2.6356 mL 6.5890 mL
15 mM 0.1757 mL 0.8785 mL 1.7571 mL 4.3927 mL
20 mM 0.1318 mL 0.6589 mL 1.3178 mL 3.2945 mL
25 mM 0.1054 mL 0.5271 mL 1.0542 mL 2.6356 mL
30 mM 0.0879 mL 0.4393 mL 0.8785 mL 2.1963 mL
40 mM 0.0659 mL 0.3295 mL 0.6589 mL 1.6473 mL
50 mM 0.0527 mL 0.2636 mL 0.5271 mL 1.3178 mL
60 mM 0.0439 mL 0.2196 mL 0.4393 mL 1.0982 mL
80 mM 0.0329 mL 0.1647 mL 0.3295 mL 0.8236 mL
100 mM 0.0264 mL 0.1318 mL 0.2636 mL 0.6589 mL
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BMS-066 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-066914946-88-6BMS066BMS 066IKKJAKIκB kinaseI kappa B kinase Janus kinaseInhibitorinhibitorinhibit

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