MLN120B

SKU: orb1219418

Description

MLN120B is a selective and ATP competitive IKKβ inhibitor (IC50: 60 nM).MLN120B almost completely blocks the stimulation of MM.1S, U266, and INA6 cell growth, as well as IL-6 secretion from BMSCs, induced by multiple myeloma cell adherence to BMSCs . MLN120B shows an inhibitory effect on LPS induced NF-κB activation in RAW267.4 cells. The IC50 values of MLN120B is 1.4, 14.8 or 27.3 μM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively.MLN120B (50 mg/kg, p.o.) inhibits human multiple myeloma cell growth in vivo. MLN120B (12 mg/kg twice daily, p.o.) inhibits paw swelling in a dose-dependent manner and offers significant protection against arthritis-induced weight loss as well as cartilage and bone erosion.

Images & Validation

−

Key Properties

−

CAS Number	783348-36-7
MW	366.8
Purity	>98% (HPLC)
Formula	C₁₉H₁₅ClN₄O₂
SMILES	O=C(C1=CC=CN=C1C)NC2=C(OC)C(Cl)=CC3=C2NC4=C3C=CN=C4
Target	IκB kinase (IKK)
Solubility	DMSO:30 mg/mL (81.78 mM);Water:Insoluble

Bioactivity

−

In Vivo

MLN120B (oral administration; 50 mg/kg; twice daily; 3 weeks) induces a reduction of shuIL-6R, marker of tumor growth, marker of tumor growth. It also leads to a rend toward prolonged survival in animals treated versus control. MLN120B (oral administration; 1-30 mg/kg; twice daily; 3 weeks)inhibits paw swelling in a dose-dependent manner and offers significant protection against arthritis-induced weight loss as well as cartilage and bone erosion. NF-κB activity in arthritic joints is also reduced after MLN120B administration. Animal model: Two-month-old female Lewis rats. Dosage: 30 mg/kg, 10 mg/kg, 3 mg/kg, or 1 mg/kg. Administration: Oral administration; twice daily; 3 weeks. Result: Protected against bone and cartilage destruction in a rat model. Animal model: SCID mice implanted with human fetal bone chips and then INA6 cells are directly injected into mice. Dosage: 50 mg/kg. Administration: Oral administration; twice daily; 3 weeks. Result: Inhibited human multiple myeloma cell growth In vivo.

In Vitro

MLB120B (0-20 μM; 90 minutes) inhibits phosphorylation and degradation of IκB in RPMI 8226 and INA6 cells; however, no significant inhibition is observed in MM.1S cells. MLB120B (1.25-20 μM; 90 minutes) completely abrogates TNF-a-induced phosphorylation and degradation of IκB in a dosedependent fashion. Phosphorylation of p65 NF-κB induced by TNF-a is also blocked by MLN120B. MLN120B inhibits proliferation of multiple myeloma cell lines. MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells. Five percent to fifty percent and 18% to 70% inhibition in proliferation is observed at doses >20 uM and [3H]thymidine uptake, respectively. MLN120B (1.25-40 μM; 72 hours) almost completely blocks stimulation of MM.1S, U266, and INA6 cell growth, as well as IL-6 secretion from BMSCs, induced by multiple myeloma cell adherence to BMSCs. MLN120B shows an inhibitory effect on LPS induced NF-κB activation in RAW267.4 cells. The IC50 values of MLN120B is 1.4 μM, 14.8 μM or 27.3 μM for NF-κB2-luc2, IL8-luc2 or TNF-AIP3-luc2 reporter transfected cells, respectively. Western blot analysis. Cell line: MM.1S cells Concentration: 1.25-20 μM Incubation time: 90 minutes. Result: Inhibited p- IκB and p-P65 expression in a dose-dependent manner. Cell Viability Assay Cell line: Multiple myeloma cell lines: MM.1S, MM.1R, RPMI 8226, RPMI-LR5, RPMI-Dox40, U266, and INA6 cells Concentration: 1.25 μM-20 μM Incubation time: 72 hours. Result: Inhibits proliferation of multiple myeloma cell lines.

Storage & Handling

−

Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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.

Quick Database Links

Gene Symbol

IκB kinase (IKK)

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

MLN120B (orb1219418)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	98.92%
CAS Number:	783348-36-7
MW:	366.8
Formula:	C₁₉H₁₅ClN₄O₂

CAS Number:	1782573-78-7
MW:	439.72
Formula:	C₁₉H₁₇Cl₃N₄O₂

MLN120B

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Similar Products

MLN120B [orb1296064]

ML 120B dihydrochloride [orb1691494]

Quality Guarantee

Quick Database Links

Documents Download

Request a Document

Protocol Information

MLN120B (orb1219418)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors