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MI-2(MALT1 inhibitor)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MI-2(MALT1 inhibitor)图片
CAS NO:1047953-91-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)455.72
FormulaC19H17Cl3N4O3
CAS No.1047953-91-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 91 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: 21 mg/mL (46.1 mM)
Solubility (In vivo)2% DMSO+30% PEG 300: 5 mg/mL
SynonymsMI-2; MI 2; MI2; MALT1 inhibitor
实验参考方法
In Vitro

In vitro activity: MI-2 inhibits MALT1 functions in ABC-DLBCL cell lines with excellent cell penetration. MI-2 produces selective growth inhibition for MALT1-dependent cell lines with GI50 of 0.2, 0.5, 0.4, and 0.4 礛 in HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells, whereas the ABC-DLBCL MALT1-independent cell lines, U2932 and HLY-1, and the two GCB-DLBCL cell lines were resistant


Kinase Assay: Ac-LRSR-AMC is used as substrate and reactions are measured with excitation/emission wavelengths of 360/465 nm. Two time points are measured for each reaction to eliminate false positives due to compound autofluorescence. The final percent inhibition is calculated with the formula {[fluorescencetest compound (T2-T1)-fluorescenceneg ctrl (T2-T1)]/[fluorescencepos ctrl (T2-T1)-fluorescenceneg ctrl (T2-T1)]} × 100, where Z-VRPR-FMK (300 nM) is used as positive control and buffer only as negative control. The positive hits are validated in concentration-response experiments within a dose range of 0.122–62.5 μM to determine IC50 of the compounds. Activity is validated using recombinant full-length wild-type MALT1.


Cell Assay: Cell proliferation (MALT1-independent cell lines: U2932 and HLY-1, and the two GCB-DLBCL cell lines; MALT1-dependent cell lines: HBL-1, TMD8, OCI-Ly3, and OCI-Ly10 cells) is determined by ATP quantification using a luminescent method and trypan blue dye exclusion. Standard curves for each cell line are calculated by plotting the cell number (determined using trypan blue) against their luminescence values, and cell number is calculated accordingly. Cell viability in drug-treated cells is normalized to their respective controls (fractional viability), and results are given as 1-fractional viability. CompuSyn software is used to determine GI25 and GI50 values.

In VivoMI-2 (350 mg/kg) is nontoxic to mice. MI-2 (25 mg/kg/day i.p.) profoundly suppresses the growth of both the TMD8 and HBL-1 ABC-DLBCL xenografts, whereas it has no effect on the growth of OCI-Ly1 tumors.
Animal modelSCID NOD.CB17-Prkdcscid/J mice bearing human HBL-1, TMD8, or OCI-Ly1 xenograft.
Formulation & DosageDissolved in 5% DMSO; 25 mg/kg/day; i.p. injection
References

Cancer Cell. 2012 Dec 11;22(6):812-24.