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MLN9708

Catalog No. T2016 CAS 1201902-80-8

Synonyms: Ixazomib Citrate

MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

MLN9708, CAS 1201902-80-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 61.00
25 mg	In stock	$ 97.00
50 mg	In stock	$ 133.00
100 mg	In stock	$ 226.00
200 mg	In stock	$ 336.00
500 mg	In stock	$ 563.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 98.79%

Purity: 98.24%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 (Ixazomib Citrate) is MLN2238 in aqueous solutions or plasma.
Targets&IC50	20S proteasome:0.93 nM(Ki), 20S proteasome:3.4 nM
In vitro	MLN9708 exhibits anticancer activity in a variety of solid tumors and hematologic malignancies.
In vivo	Upon contact with aqueous solutions and plasma, MLN9708 rapidly hydrolyzes into MLN2238, which possesses bioactivity. MLN2238 inhibits the chymotrypsin-like hydrolytic sites of the 20S proteasome ([IC50=3.4 nM,Ki=0.93 nM]). It also inhibits the caspase-like ([IC50=31 nM]) and trypsin-like hydrolytic sites ([IC50=3.5 μM]) of the 20S proteasome.
Kinase Assay	Kinase assay: Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument.
Cell Research	Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37 °C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37 °C and then washed thrice in medium to remove the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37 °C, after which the medium is removed and replaced with fresh medium. (Only for Reference)

Synonyms	Ixazomib Citrate
Molecular Weight	517.12
Formula	C20H23BCl2N2O9
CAS No.	1201902-80-8

Storage

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

Solubility Information

DMSO: 93 mg/mL (179.8 mM)

References and Literature

1. Kupperman E, et al. Cancer Res, 2010, 70(5), 1970-80. 2. Chauhan D, et al. Clin Cancer Res, 2011, 17(16), 5311-21. 3. Lee EC, et al.Clin Cancer Res, 2011, 17(23),7313-23. 4. E. T. Rodler, et al. Journal of Clinical Oncology, 2010, 28(15)

Citations

1. Zhou Q, Liang J, Yang T, et al. Carfilzomib modulates tumor microenvironment to potentiate immune checkpoint therapy for cancer. EMBO Molecular Medicine. 2022 Jan 11;14(1):e14502. doi: 10.15252/emmm.202114502. Epub 2021 Dec 13.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Active Compound Library Bioactive Compound Library HIF-1 Signaling Pathway Compound Library Hematonosis Compound Library FDA-Approved & Pharmacopeia Drug Library FDA-Approved Drug Library

Related Products

Related compounds with same targets

Alloxan monohydrate TPCK Bortezomib Alogliptin Benzoate Pepstatin Cilastatin Tomatine Calpastatin subdomain B

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Keywords

MLN9708 1201902-80-8 Proteases/Proteasome Ubiquitination Proteasome MLN 9708 MLN-9708 Ixazomib Citrate inhibitor inhibit

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