BMS-345541

SKU: orb1300867

Description

BMS-345541 (IKK Inhibitor III) is a selective small molecule inhibitor targeting IKK-2 and IKK-1 catalytic subunits with IC50 values of 0.3 µM and 4 µM, respectively. It is widely used in vitro and in vivo to study NF-κB signaling in inflammation, cancer, and immune response research.

Research Area

Signal Transduction

Images & Validation

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Key Properties

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CAS Number	445430-58-0
MW	255.32
Purity	>99.99% (May vary between batches)
Formula	C₁₄H₁₇N₅
SMILES	Cc1cnc2c(NCCN)nc3ccc(C)cc3n12
Target	IκB/IKK
Solubility	Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.92 mM);DMSO:5.1 mg/mL (19.97 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	IKKβ:0.3 μM\|IKKα:4 μM
In Vivo	Treatment with 5 μM BMS-345541 induced cell cycle arrest at the G2/M phase in BE-13 and DND-41 cells and hindered RPMI-8402 cells from staying in the sub-G1 phase. This concentration, after 16 hours, led to an increase in apoptotic cells, along with time-dependent cleavage of procaspase-8, procaspase-3, and poly(ADP-ribose). Furthermore, 5 μM BMS-345541 triggered time-dependent dephosphorylation of IκBα and p65. At a concentration of 10 μM, BMS-345541 inhibited the growth of normal human epidermal melanocytes and metastatic melanoma cells (SK-MEL-5, A375, and HS294T), with inhibition rates of 96% and 99% after 72 hours, respectively. This dosage also reduced IKK activity by 76%, NF-kB activity by 95%, and diminished CXCL1 production. Dose-dependently, BMS-345541 inhibited the phosphorylation of IκBα stimulated by TNF-α in THP-1 monocytes, with an IC50 of 4 μM. In human umbilical vein endothelial cells, it suppressed the expression of TNFα-induced ICAM-1 and VCAM-1, with an IC50 of 5 μM. BMS-345541 binds to the allosteric sites of IKK-1 and IKK-2, affecting the activity sites of different subunits. It impacted various mitotic cell cycle transitions, including entry into mitosis, progression from early to late stages, and cytokinesis. Adding BMS-345541 to cells resulted in arrest at the G phase and inhibited the activation of Aurora A, B, and C, Cdk1, and the phosphorylation of histone H3. Treatment with BMS-34554 led to nuclear translocation of FOXO3a in T-ALL cells, including the regulation of p21 CIP1 gene expression levels. BMS-345541 also inhibited the growth of primary T-ALL cells from pediatric patients, with an IC50 of 2-6 μM. Read more...
In Vitro	Tumor-bearing mice treated with 75 mg/kg of BMS-345541 exhibited effective growth inhibition against SK-MEL-5, A375, and Hs 294T, with inhibition rates of 86%, 69%, and 67%, respectively, compared to the control group. At a dosage of 100 mg/kg, BMS-345541 reduced cumulative arthritis damage scores from 4.4 to 0, accompanied by lower degrees of tibial joint degeneration, severity of inflammation, synovial proliferation, bone absorption, and cartilage erosion. BMS-345541 dose-dependently inhibited IL-1β signaling, with animals in the 100 mg/kg dosage group displaying levels comparable to disease-free control animals. Oral administration of 100 mg/kg BMS-345541 reduced the weight ratio, clinical intestinal scores, average damage scores, and average inflammation scores in mice induced with dextran sulfate sodium colitis, which were 0.86 (vs the control group’s 0.77), 1.0 (vs the control group’s 2.5), 5.66 (vs the control group’s 8.52), and 6.82 (vs the control group’s 12.33), respectively. Read more...
Cell Research	1×105 cells per well are plated in six-well plates with 10% fetal bovine serum medium overnight to allow cell adhesion. Cells ae cultured in medium containing BMS-345541 for 72 hours of treatment. Cells are counted with a hemocytometer.(Only for Reference) Read more...

Storage & Handling

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Storage	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.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BMS345541, BMS-345541, BMS-345541 free base, BMS 345541, IκB kinase, IκB, I kappa B kinase, IKK2, IkB/IKK, IkB, IKK Inhibitor III, IKK1, IKK

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Compound Identifiers

PubChem CID

9813758 ↗

Key Properties

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No computed properties available.

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BMS-345541 (orb1300867)

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Purity:	99.92%
CAS Number:	547757-23-3
MW:	291.78
Formula:	C₁₄H₁₈ClN₅

Purity:	>98% (HPLC)
CAS Number:	445430-58-0
MW:	255.3183
Formula:	C₁₄H₁₇N₅

BMS-345541

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

BMS-345541 hydrochloride [orb1298849]

BMS-345541 free base [orb1225032]

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BMS-345541 (orb1300867)

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