Skip to main content

Table 1 SERCA inhibitors

From: Targeting oncogenic Notch signaling with SERCA inhibitors

Structure

Compound

Binding site

IC50 (μM)

Cell line/in vivo

References

Clinical trial

Artemisinin

Leu263, Phe264, Gln267, Ile977, Ile981, Ala985, Asn1039, Leu1040, Ile1041 and Asn1042 (*)

9.6

Breast cancer

[109]

N/A

> 40

NSCLC

[110]

> 60

Prostate cancer

[111]

> 60

Renal cancer

> 60

Ovarian cancer

12–60

Leukemia

101–(> 1000)

Melanoma

[112]

> 50

Neuroblastoma

156–204

Colon cancer

31–(> 1000)

Pancreas cancer

9.7

HCC

[113]

CAD204520

Asp59 (M1), Val62 (M1), Asn101 (M2), Asp254 (M3), Pro312 (M4)

2.1–9.9

T-ALL

[114]

N/A

1.4–12.7

MCL

N/A

T-ALL xenografted model

Casearin J

N/A

0.7–2.5

T-ALL

[115, 116]

N/A

Curcumin

Hydrophobic task between M3 and M5

7–15

Purified SERCA

[117]

NCT02064673

NCT04403568

NCT04266275

NCT01490996

NCT00094445

50

Glioblastoma

[118]

10–20

Colorectal cancer

[119]

10–20

B-ALL

[120]

15 ± 6.8–25 ± 5.2

Cervical cancer

[121]

11.31 ± 1.47

Breast cancer

[122]

5.5–11.6

HNSCC

[123]

N/A

Liposarcoma xenografted model

[124]

View full size image

CXL017

N/A

1.04

NCI-60 cancer cell line panel

[125]

N/A

13.5 ± 0.5

AML

[126]

Cyclopiazonic acid

Gln56 (M1), Asp59 (M1), Asn101 (M2), hydrophobic indole group (M3, M4)

0.175

AML

[127]

N/A

0.125

Renal carcinoma

0.09 (SERCA1b)

2.5 (SERCA2b)

0.6 (SERCA3a)

Purified SERCA

[50]

14.76–17.84

T-ALL

[35]

DBHQ

Asp59 (M1), Pro308 (M4)

7 ± 4 (SERCA1b)

2.6 ± 1.3 (SERCA2b)

1.7 ± 1 (SERCA3a)

Purified SERCA

[50]

N/A

sHA 14–1

N/A

29.2 ± 4.9 (SERCA1a)

23.5 ± 4.2 (SERCA2b)

Purified SERCA

[128]

N/A

50

B-ALL

Thapsigargin

Phe256 (M3); Ile765 (M5); Tyr837 (M7)

2.1 × 10–4 (SERCA1b)

1.3 × 10–3 (SERCA2b)

0.012 (SERCA3a)

Purified SERCA

[50]

N/A

0.007 ± 0.001–3 ± 1

AML

[126]

Ì´4

Adrenocortical carcinoma (ACC)

[129]

N/A

ACC xenografted model

3.7 × 10–4-14.67

NSCLC

[35, 130]

0.13–3.94

AML

5.5 × 10–4-0.026

Breast cancer

0.021

Cervix cancer

1.7 × 10–3

Melanoma

1.8 × 10–3-0.038

T-ALL

7.8 × 10–3-0.011

Prostate cancer

N/A

Drosophila intestinal stem cell model

N/A

T-ALL xenografted model

  1. (*)The binding site of artemisinin is referred to PfATP6 on Plasmodium Falciparum based on computational analysis and docking simulations [131, 132]