5.32758

IRE1α Inhibitor, MKC-3946

• 同義詞: IRE1α Inhibitor, MKC-3946, XBP1 expression blocker, MKC3946, MKC 3946
• 經驗公式（希爾表示法）: C₂₁H₂₀N₂O₃S
• CAS號碼: 1093119-54-0
• 分子量：: 380.46
• MDL號碼: MFCD30496700
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥97% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: dark yellow
• 溶解度: DMSO: 25 mg/mL
• 儲存溫度: −20°C
• SMILES 字串: [s]1c(ccc1C(=O)N4CCN(CC4)C)c2cc3c(c(c(cc3)O)C=O)cc2
• InChI: 1S/C21H20N2O3S/c1-22-8-10-23(11-9-22)21(26)20-7-6-19(27-20)15-2-4-16-14(12-15)3-5-18(25)17(16)13-24/h2-7,12-13,25H,8-11H2,1H3

描述

一般說明

A cell-permeable compound that binds to the endoribnuclease domain of IRE1α and inhibits its activity. Blocks XBP1 mRNA splicing in RPMI 8226 human multiple myeloma cells.

A cell-permeable naphthaldehyde derived compound that binds to the endoribnuclease domain of inositol requiring enzyme1α (IRE1α) to inhibit its activity and blocks X-box binding protein 1 (XBP1) mRNA splicing in RPMI 8226 human multiple myeloma (MM) cells. Down-regulates SEC61A1, p58IPK, and ERdj4 genes that are targeted by XBP1. Also shown to block XBP1s expression induced by tunicamycin without affecting the phosphorylation of IRE1a (50 mg/kg, i.p). Shown to enhance bortezomib (Cat. No. 504314) and 17-AAG (Cat. No, 100068) induced toxicity and apoptosis in RPMI8226 and INA6 cells. However, it does not have any significant effect on normal mononuclear cells. Suppresses the growth of RPMI 8226 xenografts in a model of human MM in mice (50 mg/kg, i.p.).

A cell-permeable naphthaldehyde derived compound that binds to the endoribnuclease domain of inositol requiring enzyme1α (IRE1α) to inhibit its activity and blocks X-box binding protein 1 (XBP1) mRNA splicing in RPMI 8226 human multiple myeloma (MM) cells. Down-regulates SEC61A1, p58IPK, and ERdj4 genes that are targeted by XBP1. Also shown to block XBP1s expression induced by tunicamycin without affecting the phosphorylation of IRE1a (50 mg/kg, i.p). Shown to enhance bortezomib (Cat. No. 504314) and 17-AAG (Cat. No, 100068) induced toxicity and apoptosis in RPMI8226 and INA6 cells. However, it does not have any significant effect on normal mononuclear cells. Suppresses the growth of RPMI 8226 xenografts in a model of human MM in mice (50 mg/kg, i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化／生理作用

Cell permeable: yes

Primary Target
IRE1

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Mimura, N., et al. 2012. Blood.119, 5772.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable