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. 2022 Mar 22;2(4):839–852. doi: 10.1021/jacsau.1c00573

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
a

From HCHT imaging of HK cells incubated first with

b

inhibitors I at varied concentrations for 1 h and then with

c

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.

d

Conditions: P = pre-incubation: I removed before addition of T. C = co-incubation: I not removed before addition of T.

e

Concentration needed to reach 15% inhibition.

f

Concentration needed to reach 50% inhibition. SEM ≤ 30%.

g

Concentration needed to lower relative viability (RV) by 50%. RV: number of PI negative cells divided by HOE-positive cells. SEM ≤ 30%.

h

Data from ref (51).

i

Data from ref (52).

j

Data from ref (79).