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BMS-066

Catalog No. T14669 CAS 914946-88-6

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

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BMS-066, CAS 914946-88-6

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 2,420.00
50 mg	10-14 weeks	$ 3,180.00
100 mg	10-14 weeks	$ 4,300.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
Targets&IC50	TYK2:72 nM, IKKβ:9 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	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. The joints from animals receiving 10 mg/kg BMS-066 are normal or show minimal changes in both inflammation and bone resorption. Bone density measurements also show a clear dose-dependent benefit of treatment with BMS-066. 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. 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].

Molecular Weight	379.42
Formula	C19H21N7O2
CAS No.	914946-88-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Gillooly KM, et al. Periodic, partial inhibition of IkappaB Kinase beta-mediated signaling yields therapeutic benefit in preclinical models of rheumatoid arthritis. J Pharmacol Exp Ther. 2009 Nov;331(2):349-60. 2. Tokarski JS, et al. Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain. J Biol Chem. 2015 Apr 24;290(17):11061-74.

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Keywords

BMS-066 914946-88-6 NF-Κb Tyrosine Kinase/Adaptors IκB/IKK Tyrosine Kinases BMS 066 BMS066 inhibitor inhibit

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