Table 2. Inhibition of Cytosolic Deliverya.
Ib | Tc | condd | MICe (μM) | IC50f (μM) | RV50g (μM) | |
---|---|---|---|---|---|---|
1h | 2 | 31 | P | 800 | >5000 | 4400 |
2 | 2 | 28 | P | >50 | >100 | >100 |
3h | 3 | 31 | P | 200 | >1000 | 1300 |
4 | 3 | 28 | P | 5 | 60 | >1000 |
5i | 3 | 32 | P | 250 | 550 | |
6 | 3 | 31 | C | 3 | 35 | >1000 |
7 | 15 | 31 | C | 1.5 | 22 | >500 |
8 | 11 | 31 | P | 1.5 | 9 | >20 |
9 | 11 | 31 | C | <5 | >50 | >50 |
10 | 11 | 28 | C | <1 | >50 | >50 |
11 | 12 | 31 | C | <1 | 7 | >50 |
12 | 12 | 28 | C | 5 | 60 | 100 |
13 | 4 | 28 | C | 0.3 | ≈15 | >5 |
14 | 33 | 28 | C | 1 | >5 | >5 |
15 | 34 | 31 | P | 3 | >100 | >100 |
16 | 34 | 31 | C | 16 | >100 | >100 |
17 | 34 | 28 | C | 1 | 26 | >50 |
18 | 35 | 31 | C | 9 | 51 | >100 |
19 | 35 | 28 | C | 4 | 25 | >50 |
20 | 45 | 31 | P | <1 | 10 | >20 |
21 | 45 | 31 | C | 2 | 8 | >20 |
22i | 45 | 32 | P | >100 | >100 | |
23 | 45 | 28 | P | 1 | 8 | >20 |
24 | 36 | 31 | C | 2 | 27 | >50 |
25 | 37 | 31 | C | 7 | ≈60 | >50 |
26 | 38 | 31 | C | 23 | 47 | >50 |
27 | 39 | 31 | C | 14 | ≈60 | >50 |
28 | 40 | 31 | C | 8 | 50 | >50 |
29 | 46 | 31 | C | <2 | 49 | >100 |
30h | 47 | 31 | P | ≤0.1 | 1.3 | 35 |
31 | 47 | 28 | P | >10 | >10 | >10 |
32i | 47 | 32 | P | 2 | 50 | |
33j | 48 | 31 | P | <1 | 4 | >20 |
34j | 49 | 31 | P | 4 | 40 | 60 |
35i | 49 | 32 | P | 0.3 | 10 | |
36 | 49 | 28 | P | 9 | 53 | >50 |
37 | 41 | 28 | C | 1 | 8 | >50 |
38 | 42 | 28 | P | 2 | 5 | 22 |
39 | 43 | 28 | P | 4 | >50 | 43 |
40 | 44 | 28 | P | 4 |
From HCHT imaging of HK cells incubated first with
inhibitors I at varied concentrations for 1 h and then with
transporters T at the constant concentration (28, 5 μM; 31, 10 μM; 32, 0.5 or 1 μM) for 30 min, reporting fluorescence intensity of T inside intact, PI negative cells.
Conditions: P = pre-incubation: I removed before addition of T. C = co-incubation: I not removed before addition of T.
Concentration needed to reach 15% inhibition.
Concentration needed to reach 50% inhibition. SEM ≤ 30%.
Concentration needed to lower relative viability (RV) by 50%. RV: number of PI negative cells divided by HOE-positive cells. SEM ≤ 30%.
Data from ref (51).
Data from ref (52).
Data from ref (79).