BDBM411364 US10774056, Compound 070 US11542242, Compound 070 US10385031, Compound 070
BDBM271759 US10065941, Compound R-070 US9732060, Compound R-070
BDBM476920 US11345716, Compound II-070 US10870660, Compound II-070
US10065941, Compound I-070 BDBM271569 US9732060, Compound I-070
US10870660, Compound I-070 US11345716, Compound I-070 BDBM476880
BDBM105560 US8575197, I-070
BDBM184436 US9150578, I-070
BDBM230226 US9340500, I-070
BDBM235460 US9359338, Exe. 070
BDBM550222 US11306081, Example 070
BDBM586152 US11530244, Compound 070
BDBM588355 US11542274, Compound 070
BDBM716632 US20250034135, Compound 070
BDBM719157 US20250051277, Compound 070
BDBM730857 US20250122183, Example 070
BDBM733664 US20250115609, Compound 070
US8575197, II-070 BDBM106127
US9212130, I-070 BDBM196193
BDBM152163 US8987474, HL2-070-1
BDBM152164 US8987474, HL2-070-2
BDBM152165 US8987474, HL2-070-3
BDBM152166 US8987474, HL2-070-4
BDBM152168 US8987474, HL2-070-6
BDBM152169 US8987474, HL2-070-7
BDBM152170 US8987474, HL2-070-9
BDBM306861 US10150728, Example I-070
BDBM50465914 Branaplam LMI-070 LMI070
BDBM593787 US11578084, Compound I-070
BDBM601820 US11643396, Example MA1-070
BDBM640525 US20230399319, Example 2-070
BDBM661800 US20240101572, Example 2-070
BDBM731352 US12281099, Example I-070
US12247004, Compound ANASIA-070 BDBM726215
US20230286948, Compound HYBI-070 BDBM617679
US20240083872, Compound I-070 BDBM657860
US20240383900, Compound PPA-070 BDBM706406
US20250026765, Compound I-070 BDBM715463
US20250092056, Compound I-070 BDBM728468
US9550763, Compound I-070 BDBM244321
BDBM152170 BDBM152167 US8987474, HL2-070-5
US11643396, Example SG2-070-01 BDBM601813
BDBM710612 US12187701, Compound FMF-05-070-1
US10202389, Compound I-070 US9796725, Compound I-070 US9663525, Compound I-070 (rac)-((1R,2R,3S,4R)-4-(2-(4-fluoro-2-methoxyphenyl)pyrazolo[1,5-a]pyrimidin-7- BDBM329862
CHEMBL302625 US9120744, CDE-070 BDBM50058812 N,N'-1,3-Propanediylbis(3,4,5-trihydroxybenzamide)Hydrate
BDBM346043 4-{2-[6-Methyl-2-(3- trifluoromethyl- phenyl)-3H- benzoimidazol-5- ylamino]-thiazol-4- yl}-benzonitrile US10202370, Example 070
2-[1H-benzimidazol-2-yl-(5-fluoro- 2-hydroxy-phenyl)methyl]-8-fluoro- 6-[4-(1-methyl-4-piperidyl)phenyl]- isoquinolin-1-one; hydrochloride BDBM765185 US12391671, Compound 070
- Nguyen, M; Marcellus, RC; Roulston, A; Watson, M; Serfass, L; Murthy Madiraju, SR; Goulet, D; Viallet, J; Bélec, L; Billot, X; Acoca, S; Purisima, E; Wiegmans, A; Cluse, L; Johnstone, RW; Beauparlant, P; Shore, GC Small molecule obatoclax (GX15-070) antagonizes MCL-1 and overcomes MCL-1-mediated resistance to apoptosis. Proc Natl Acad Sci U S A 104: 19512-7 (2007)
- Evaluation of NLRP3 Inflammasome Inhibitory Activity Assay The NLRP3 inflammasome inhibitory activity of test compounds were evaluated CM the basis of the inhibitory activity of the IL-1β, production in THP1-Null cells (Product Number: thp-null, InvivoGen). Cells were maintained for culture in RPMI-1640 media containing 10% (v/v) fetal bovine serum, 25 mmol/1. RUES, 100 U/mL penicillin, 100 μg/mL streptomycin, 100 μg/ml normocin, and 200 μg/mL hygromycin B (set at 37° C., 5% CO2/95% air). Cells were suspended with media for assay containing 0.5 μmol/L PMA (RPMI-1640 media containing 10% (v/v) fetal bovine serum, 100 U/mL penicillin, and 100 μg/mL streptomycin), and the suspended cells were seeded on Corning (registered trademark) 384-well Flat. Clear Bottom Black Polystyrene TC-treated Microplates (25,000 cells/25 μL/well)(followed by incubation (set at 37° C., 5% CO2/95% air) overnight supernatant of the culture was removed, and thereto was added media for assay (25 UL/well) containing 1 μg/mL Lipopolysaccharides (Product Number: L2654, Sigma-Aldrich (registered trademark)). Then, the culture was further incubated for 3 hours (set at 37° C., 5% CO2/91% air). The supernatant of the culture was removed. Then, a vehicle solution prepared from Opti-MEM (trademark) medium (Product Number: 31985-070, Invitrogen) was added to blank-setting wells and control-setting wells (20 μL/well), followed by incubation for 15 minutes (set at 37° C., 5% CO2/91% air). A solution containing a test compound (20 μL/well) was added to test compound-setting wells. Further, Opti-MEM (trademark) medium containing Nigericin (Product Number: N7143, Sigma-Aldrich (registered trademark)) was added to the control-setting wells and test compound-setting wells (5 μL/well), followed by incubation for 1.5 hours (set at 37° C., 5% CO2/95% air). The final concentration of Nigericin was adjusted to be 7.5 μmol/L, 5 μL/well of Opti-MEM (trademark) medium was added to the blank setting wells. The supernatant of the culture was cryonically stored (set at −20° C.) until measurement of IL-1β.
- Evaluation of NLRP3 Inflammasome Inhibitory Activity Assay The NLRP3 inflammasome inhibitory activity of test compounds were evaluated on the basis of the inhibitory activity of the IL-1β production in THP1-Null cells (Product Number: thp-null, InvivoGen). Cells were maintained for culture in RPMI-1640 media containing 10% (v/v) fetal bovine serum, 25 mmol/L HEPES, 100 U/mL penicillin, 100 μg/mL streptomycin, 100 μg/mL normocin, and 200 μg/mL hygromycin B (set at 37° C., 5% CO2/95% air). Cells were suspended with media for assay containing 0.5 μmol/L PMA (RPMI-1640 media containing 10% (v/v) fetal bovine serum, 100 U/mL penicillin, and 100 μg/mL streptomycin), and the suspended cells were seeded on Corning (registered trademark) 384-well Flat Clear Bottom Black Polystyrene TC-treated Microplates (25,000 cells/25 μL/well), followed by incubation (set at 37° C., 5% CO2/95% air) overnight. The supernatant of the culture was removed, and thereto was added media for assay (25 μL/well) containing 1 μg/mL Lipopolysaccharides (Product Number: L2654, Sigma-Aldrich (registered trademark)). Then, the culture was further incubated for 3 hours (set at 37° C., 5% CO2/95% air). The supernatant of the culture was removed. Then, a vehicle solution prepared from Opti-MEM (trademark) medium (Product Number: 31985-070, Invitrogen) was added to blank-setting wells and control-setting wells (20 μL/well), followed by incubation for 15 minutes (set at 37° C., 5% CO2/95% air). A solution containing a test compound (20 μL/well) was added to test compound-setting wells. Further, Opti-MEM (trademark) medium containing Nigericin (Product Number: N7143, Sigma-Aldrich (registered trademark)) was added to the control-setting wells and test compound-setting wells (5 μL/well), followed by incubation for 1.5 hours (set at 37° C., 5% CO2/95% air). The final concentration of Nigericin was adjusted to be 7.5 μmol/L. 5 μL/well of Opti-MEM (trademark) medium was added to the blank-setting wells. The supernatant of the culture was cryonically stored (set at −20° C.) until measurement of IL-1β.