2. GPCR/G Protein Immunology/Inflammation NF-κB Apoptosis
  3. Leukotriene Receptor NO Synthase NF-κB COX TNF Receptor Interleukin Related
  4. Tryptanthrin

Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.

For research use only. We do not sell to patients.

Tryptanthrin

Tryptanthrin Chemical Structure

CAS No. : 13220-57-0

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Tryptanthrin:

Tryptanthrin Related Antibodies

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

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nNOS iNOS eNOS

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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COX COX-1 COX-2 COX-3

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α[1][2].

IC50 & Target[1]

IL-2

 

nNOS

 

IL-6

 

IL-10

 

IL-12

 

Cellular Effect
Cell Line Type Value Description References
A-431 IC50
9 3
Compound: 47
Anticancer activity against human A-431 cells assessed as reduction of cell viability incubated for 48 hrs by MTT assay
Anticancer activity against human A-431 cells assessed as reduction of cell viability incubated for 48 hrs by MTT assay
[PMID: 36375335]
A-431 IC50
9 3
Compound: 47
Anticancer activity against human A-431 cells assessed as reduction of cell viability incubated for 48 hrs by MTT assay
Anticancer activity against human A-431 cells assessed as reduction of cell viability incubated for 48 hrs by MTT assay
[PMID: 36375335]
A498 GI50
0.95 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against renal A498 human cancer cell lines
Tested for in vitro cytotoxic activity against renal A498 human cancer cell lines
[PMID: 12161121]
A498 GI50
0.95 3
Compound: 47
Growth inhibition of human A498 cells by SRB method
Growth inhibition of human A498 cells by SRB method
[PMID: 36375335]
A498 GI50
0.95 3
Compound: 1; Try
Growth inhibition of human A498 cells assessed as reduction in cell viability
Growth inhibition of human A498 cells assessed as reduction in cell viability
[PMID: 38665827]
A498 GI50
0.95 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against renal A498 human cancer cell lines
Tested for in vitro cytotoxic activity against renal A498 human cancer cell lines
[PMID: 12161121]
A498 GI50
0.95 3
Compound: 47
Growth inhibition of human A498 cells by SRB method
Growth inhibition of human A498 cells by SRB method
[PMID: 36375335]
CCRF-CEM GI50
14.47 3
Compound: Tryptanthrin
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
[PMID: 32712536]
CCRF-CEM IC50
44.36 3
Compound: Tryptanthrin
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
[PMID: 32712536]
A549 IC50
74.71 3
Compound: 1; Try
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
[PMID: 38665827]
A549 IC50
74.71 3
Compound: 1; Try
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
DU-145 GI50
0.4 3
Compound: 47
Growth inhibition of human DU-145 cells by sulforhodamine B assay
Growth inhibition of human DU-145 cells by sulforhodamine B assay
[PMID: 36375335]
DU-145 GI50
0.4 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against prostate DU145 human cancer cell lines
Tested for in vitro cytotoxic activity against prostate DU145 human cancer cell lines
[PMID: 12161121]
A549 IC50
8.25 3
Compound: 1; Try
Antiproliferative activity against human A549 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated by 48 hrs by MTT assay
[PMID: 38665827]
A549 IC50
> 100 3
Compound: 1; Try
Antiproliferative activity against human A549 cells assessed as inhibition of cell viability
Antiproliferative activity against human A549 cells assessed as inhibition of cell viability
[PMID: 38665827]
DU-145 IC50
6.22 3
Compound: 1a
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
[PMID: 22819942]
HCT-15 IC50
8.49 3
Compound: 1a
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
[PMID: 22819942]
A549 IC50
> 150 3
Compound: 1; Try
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
Antiproliferative activity against human A549 cells assessed as cell growth inhibition
[PMID: 38665827]
A549/CDDP IC50
> 100 3
Compound: 1; Try
Antiproliferative activity against human A549/DDP cells assessed as inhibition of cell viability
Antiproliferative activity against human A549/DDP cells assessed as inhibition of cell viability
[PMID: 38665827]
HEK293 IC50
4.11 3
Compound: 1a
Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay
Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay
[PMID: 22819942]
HEK293 IC50
0.0537 3
Compound: 5a, Tryptanthrin
Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
[PMID: 24099220]
Bel-7402 IC50
41.29 3
Compound: 1; Try
Antiproliferative activity against human Bel-7402 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human Bel-7402 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
CCRF-CEM GI50
14.47 3
Compound: Tryptanthrin
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
[PMID: 32712536]
HEK293 IC50
0.14 3
Compound: 5a
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
[PMID: 30321802]
HepG2 IC50
305.4 14
Compound: tryptanthrin
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 25654185]
CCRF-CEM IC50
44.36 3
Compound: Tryptanthrin
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
Antiproliferative activity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by eosin exclusion dye based light microscopic method
[PMID: 32712536]
HL-60 IC50
5 3
Compound: TBr; 1a
Antiproliferative activity against human HL60 cells after 24 hrs
Antiproliferative activity against human HL60 cells after 24 hrs
[PMID: 28720329]
HL-60 IC50
2 3
Compound: TBr; 1a
Antiproliferative activity against human HL60 cells after 48 hrs
Antiproliferative activity against human HL60 cells after 48 hrs
[PMID: 28720329]
Huh-7 CC50
>10 3
Compound: GNF-Pf-2691
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
[PMID: 18579783]
DU-145 GI50
0.4 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against prostate DU145 human cancer cell lines
Tested for in vitro cytotoxic activity against prostate DU145 human cancer cell lines
[PMID: 12161121]
K562 IC50
15 3
Compound: TBr; 1a
Antiproliferative activity against human K562 cells after 24 hrs
Antiproliferative activity against human K562 cells after 24 hrs
[PMID: 28720329]
DU-145 GI50
0.4 3
Compound: 1; Try
Growth inhibition of human DU-145 cells assessed as reduction in cell viability
Growth inhibition of human DU-145 cells assessed as reduction in cell viability
[PMID: 38665827]
K562 IC50
5 3
Compound: TBr; 1a
Antiproliferative activity against human K562 cells after 48 hrs
Antiproliferative activity against human K562 cells after 48 hrs
[PMID: 28720329]
K562 IC50
8.8 6
Compound: TBr; 1a
Antiproliferative activity against human K562 cells after 48 hrs by MTT staining-based method
Antiproliferative activity against human K562 cells after 48 hrs by MTT staining-based method
[PMID: 28720329]
DU-145 GI50
0.4 3
Compound: 47
Growth inhibition of human DU-145 cells by sulforhodamine B assay
Growth inhibition of human DU-145 cells by sulforhodamine B assay
[PMID: 36375335]
DU-145 IC50
6.22 3
Compound: 1a
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
[PMID: 22819942]
K562 IC50
6.3 6
Compound: 47
Cytotoxicity against human K562 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human K562 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 36375335]
M14 GI50
15 3
Compound: 47
Growth inhibition of human M14 cells
Growth inhibition of human M14 cells
[PMID: 36375335]
HCT-116 IC50
17.49 3
Compound: 1; Try
Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
M14 GI50
15 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against melanoma M14 human cancer cell lines
Tested for in vitro cytotoxic activity against melanoma M14 human cancer cell lines
[PMID: 12161121]
MCF7 IC50
11.1 3
Compound: 7
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
[PMID: 18507473]
HCT-15 IC50
8.49 3
Compound: 1a
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
[PMID: 22819942]
MCF7 IC50
0.58 3
Compound: TBr; 1a
Cytotoxicity against human wild-type MCF7 cells after 72 hrs
Cytotoxicity against human wild-type MCF7 cells after 72 hrs
[PMID: 28720329]
HEK293 IC50
0.0537 3
Compound: 5a, Tryptanthrin
Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
[PMID: 24099220]
HEK293 IC50
0.14 3
Compound: 5a
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
[PMID: 30321802]
MOLT-4 IC50
10 3
Compound: TBr; 1a
Antiproliferative activity against human MOLT4 cells after 24 hrs
Antiproliferative activity against human MOLT4 cells after 24 hrs
[PMID: 28720329]
HEK293 IC50
4.11 3
Compound: 1a
Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay
Cytotoxicity against human HEK293 cells after 72 hrs by MTT assay
[PMID: 22819942]
MOLT-4 IC50
8 3
Compound: TBr; 1a
Antiproliferative activity against human MOLT4 cells after 48 hrs
Antiproliferative activity against human MOLT4 cells after 48 hrs
[PMID: 28720329]
NCI/ADR-RES GI50
30 3
Compound: 47
Growth inhibition of human MCF7ADR cells
Growth inhibition of human MCF7ADR cells
[PMID: 36375335]
NCI/ADR-RES GI50
30 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against breast MCF-7/ADR human cancer cell lines
Tested for in vitro cytotoxic activity against breast MCF-7/ADR human cancer cell lines
[PMID: 12161121]
NCI/ADR-RES IC50
0.03 3
Compound: TBr; 1a
Cytotoxicity against human MCF7/ADR cells after 72 hrs
Cytotoxicity against human MCF7/ADR cells after 72 hrs
[PMID: 28720329]
NCI-H460 IC50
9 3
Compound: 7
Cytotoxicity against human NCI-H460 cells
Cytotoxicity against human NCI-H460 cells
[PMID: 18507473]
HL-60 IC50
2 3
Compound: TBr; 1a
Antiproliferative activity against human HL60 cells after 48 hrs
Antiproliferative activity against human HL60 cells after 48 hrs
[PMID: 28720329]
NCI-H522 GI50
15 3
Compound: 47
Growth inhibition of human NCI-H522 cells
Growth inhibition of human NCI-H522 cells
[PMID: 36375335]
HL-60 IC50
5 3
Compound: TBr; 1a
Antiproliferative activity against human HL60 cells after 24 hrs
Antiproliferative activity against human HL60 cells after 24 hrs
[PMID: 28720329]
NCI-H522 GI50
15 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against lung H522 human cancer cell lines
Tested for in vitro cytotoxic activity against lung H522 human cancer cell lines
[PMID: 12161121]
SF-268 IC50
24.4 3
Compound: 7
Cytotoxicity against human SF268 cells
Cytotoxicity against human SF268 cells
[PMID: 18507473]
HeLa IC50
> 150 3
Compound: 1; Try
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition
Antiproliferative activity against human HeLa cells assessed as cell growth inhibition
[PMID: 38665827]
SH-SY5Y IC50
22 3
Compound: 47
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability
[PMID: 36375335]
HepG2 IC50
305.4 14
Compound: tryptanthrin
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
[PMID: 25654185]
SK-N-DZ IC50
14 3
Compound: 47
Anticancer activity against human SK-N-DZ cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis
Anticancer activity against human SK-N-DZ cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis
[PMID: 36375335]
HepG2 IC50
9.51 3
Compound: 1; Try
Antiproliferative activity against human HepG2 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated by 48 hrs by MTT assay
[PMID: 38665827]
SK-OV-3 GI50
2.5 3
Compound: 47
Growth inhibition of human SK-OV-3 cells by sulforhodamine B assay
Growth inhibition of human SK-OV-3 cells by sulforhodamine B assay
[PMID: 36375335]
HepG2 IC50
90.14 3
Compound: 1; Try
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth
[PMID: 38665827]
SK-OV-3 GI50
2.5 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against ovarian SKOV3 human cancer cell lines
Tested for in vitro cytotoxic activity against ovarian SKOV3 human cancer cell lines
[PMID: 12161121]
SW-620 GI50
5 3
Compound: 47
Growth inhibition of human SW620 cells
Growth inhibition of human SW620 cells
[PMID: 36375335]
HepG2 IC50
90.14 3
Compound: 1; Try
Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
SW-620 GI50
5 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against colon SW620 human cancer cell lines
Tested for in vitro cytotoxic activity against colon SW620 human cancer cell lines
[PMID: 12161121]
T47D IC50
14.29 3
Compound: 1a
Cytotoxicity against human T47D cells after 72 hrs by MTT assay
Cytotoxicity against human T47D cells after 72 hrs by MTT assay
[PMID: 22819942]
Huh-7 CC50
> 10 3
Compound: GNF-Pf-2691
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
[PMID: 18579783]
U-251 GI50
100 3
Compound: 47
Growth inhibition of human U-251 cells
Growth inhibition of human U-251 cells
[PMID: 36375335]
U-251 GI50
100 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against CNS U251 human cancer cell lines
Tested for in vitro cytotoxic activity against CNS U251 human cancer cell lines
[PMID: 12161121]
U-87MG ATCC IC50
5 3
Compound: 5a
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
[PMID: 27475108]
U-87MG ATCC IC50
0.194 3
Compound: 5a
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
[PMID: 30321802]
U-937 IC50
3.1 6
Compound: 47
Cytotoxicity against human U-937 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human U-937 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 36375335]
K562 IC50
12.04 3
Compound: 1; Try
Antiproliferative activity against human K562 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human K562 cells incubated by 48 hrs by MTT assay
[PMID: 38665827]
K562 IC50
15 3
Compound: TBr; 1a
Antiproliferative activity against human K562 cells after 24 hrs
Antiproliferative activity against human K562 cells after 24 hrs
[PMID: 28720329]
Vero IC50
>8 6
Compound: 1a, Tryptanthrin
Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
[PMID: 23360475]
Vero IC50
>100 6
Compound: 2
Cytotoxicity against African green monkey Vero cells by CellTiter 96 aqueous nonradioactive cell proliferation assay
Cytotoxicity against African green monkey Vero cells by CellTiter 96 aqueous nonradioactive cell proliferation assay
[PMID: 30295480]
K562 IC50
5 3
Compound: TBr; 1a
Antiproliferative activity against human K562 cells after 48 hrs
Antiproliferative activity against human K562 cells after 48 hrs
[PMID: 28720329]
K562 IC50
6.3 6
Compound: 47
Cytotoxicity against human K562 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human K562 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 36375335]
K562 IC50
8.8 6
Compound: TBr; 1a
Antiproliferative activity against human K562 cells after 48 hrs by MTT staining-based method
Antiproliferative activity against human K562 cells after 48 hrs by MTT staining-based method
[PMID: 28720329]
L02 IC50
90.12 3
Compound: 1; Try
Antiproliferative activity against human HL7702 cells assessed as inhibition of cell growth
Antiproliferative activity against human HL7702 cells assessed as inhibition of cell growth
[PMID: 38665827]
L02 IC50
90.12 3
Compound: 1; Try
Antiproliferative activity against human HL7702 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HL7702 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
L02 IC50
> 100 3
Compound: 1; Try
Antiproliferative activity against human HL7702 cells assessed as inhibition of cell viability
Antiproliferative activity against human HL7702 cells assessed as inhibition of cell viability
[PMID: 38665827]
M14 GI50
15 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against melanoma M14 human cancer cell lines
Tested for in vitro cytotoxic activity against melanoma M14 human cancer cell lines
[PMID: 12161121]
M14 GI50
15 3
Compound: 1; Try
Growth inhibition of human M14 cells assessed as reduction in cell viability
Growth inhibition of human M14 cells assessed as reduction in cell viability
[PMID: 38665827]
M14 GI50
15 3
Compound: 47
Growth inhibition of human M14 cells
Growth inhibition of human M14 cells
[PMID: 36375335]
MC3T3-E1 IC50
> 100 3
Compound: 1; Try
Antiproliferative activity against mouse MC3T3-E1 cells
Antiproliferative activity against mouse MC3T3-E1 cells
[PMID: 38665827]
MCF7 IC50
0.58 3
Compound: TBr; 1a
Cytotoxicity against human wild-type MCF7 cells after 72 hrs
Cytotoxicity against human wild-type MCF7 cells after 72 hrs
[PMID: 28720329]
MCF7 IC50
11.1 3
Compound: 7
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
[PMID: 18507473]
MCF7 IC50
94.2 3
Compound: 1; Try
Antiproliferative activity against human MCF7 cells
Antiproliferative activity against human MCF7 cells
[PMID: 38665827]
MDA-MB-231 IC50
> 100 3
Compound: 1; Try
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
MGC-803 IC50
70.19 3
Compound: 1; Try
Antiproliferative activity against human MGC-803 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
MOLT-4 IC50
10 3
Compound: TBr; 1a
Antiproliferative activity against human MOLT4 cells after 24 hrs
Antiproliferative activity against human MOLT4 cells after 24 hrs
[PMID: 28720329]
MOLT-4 IC50
8 3
Compound: TBr; 1a
Antiproliferative activity against human MOLT4 cells after 48 hrs
Antiproliferative activity against human MOLT4 cells after 48 hrs
[PMID: 28720329]
NCI-H460 IC50
9 3
Compound: 7
Cytotoxicity against human NCI-H460 cells
Cytotoxicity against human NCI-H460 cells
[PMID: 18507473]
NCI-H522 GI50
15 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against lung H522 human cancer cell lines
Tested for in vitro cytotoxic activity against lung H522 human cancer cell lines
[PMID: 12161121]
NCI-H522 GI50
15 3
Compound: 1; Try
Growth inhibition of human NCI-H522 cells assessed as reduction in cell viability
Growth inhibition of human NCI-H522 cells assessed as reduction in cell viability
[PMID: 38665827]
NCI-H522 GI50
15 3
Compound: 47
Growth inhibition of human NCI-H522 cells
Growth inhibition of human NCI-H522 cells
[PMID: 36375335]
NCI/ADR-RES GI50
30 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against breast MCF-7/ADR human cancer cell lines
Tested for in vitro cytotoxic activity against breast MCF-7/ADR human cancer cell lines
[PMID: 12161121]
NCI/ADR-RES GI50
30 3
Compound: 1; Try
Growth inhibition of human MCF7ADR cells assessed as reduction in cell viability
Growth inhibition of human MCF7ADR cells assessed as reduction in cell viability
[PMID: 38665827]
NCI/ADR-RES GI50
30 3
Compound: 47
Growth inhibition of human MCF7ADR cells
Growth inhibition of human MCF7ADR cells
[PMID: 36375335]
NCI/ADR-RES IC50
0.03 3
Compound: TBr; 1a
Cytotoxicity against human MCF7/ADR cells after 72 hrs
Cytotoxicity against human MCF7/ADR cells after 72 hrs
[PMID: 28720329]
NCI/ADR-RES IC50
96.4 3
Compound: 1; Try
Antiproliferative activity against human MCF7ADR cells
Antiproliferative activity against human MCF7ADR cells
[PMID: 38665827]
PC-3 IC50
14.52 3
Compound: 1; Try
Antiproliferative activity against human PC-3 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells incubated by 48 hrs by MTT assay
[PMID: 38665827]
SF-268 IC50
24.4 3
Compound: 7
Cytotoxicity against human SF268 cells
Cytotoxicity against human SF268 cells
[PMID: 18507473]
SH-SY5Y IC50
22 3
Compound: 47
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability
[PMID: 36375335]
SK-N-DZ IC50
14 3
Compound: 47
Anticancer activity against human SK-N-DZ cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis
Anticancer activity against human SK-N-DZ cells assessed as cell growth inhibition measured after 72 hrs by DAPI staining based analysis
[PMID: 36375335]
SK-OV-3 GI50
2.5 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against ovarian SKOV3 human cancer cell lines
Tested for in vitro cytotoxic activity against ovarian SKOV3 human cancer cell lines
[PMID: 12161121]
SK-OV-3 GI50
2.5 3
Compound: 1; Try
Growth inhibition of human SK-OV-3 cells assessed as reduction in cell viability
Growth inhibition of human SK-OV-3 cells assessed as reduction in cell viability
[PMID: 38665827]
SK-OV-3 GI50
2.5 3
Compound: 47
Growth inhibition of human SK-OV-3 cells by sulforhodamine B assay
Growth inhibition of human SK-OV-3 cells by sulforhodamine B assay
[PMID: 36375335]
SK-OV-3 IC50
85.09 3
Compound: 1; Try
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell growth
[PMID: 38665827]
SW-620 GI50
5 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against colon SW620 human cancer cell lines
Tested for in vitro cytotoxic activity against colon SW620 human cancer cell lines
[PMID: 12161121]
SW-620 GI50
5 3
Compound: 1; Try
Growth inhibition of human SW620 cells assessed as reduction in cell viability
Growth inhibition of human SW620 cells assessed as reduction in cell viability
[PMID: 38665827]
SW-620 GI50
5 3
Compound: 47
Growth inhibition of human SW620 cells
Growth inhibition of human SW620 cells
[PMID: 36375335]
T-24 IC50
> 150 3
Compound: 1; Try
Antiproliferative activity against human T24 cells assessed as inhibition of cell growth
Antiproliferative activity against human T24 cells assessed as inhibition of cell growth
[PMID: 38665827]
T-24 IC50
> 150 3
Compound: 1; Try
Antiproliferative activity against human T24 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human T24 cells measured after 48 hrs by MTT assay
[PMID: 38665827]
T47D IC50
14.29 3
Compound: 1a
Cytotoxicity against human T47D cells after 72 hrs by MTT assay
Cytotoxicity against human T47D cells after 72 hrs by MTT assay
[PMID: 22819942]
U-251 GI50
100 3
Compound: 1 (Tryptanthrine)
Tested for in vitro cytotoxic activity against CNS U251 human cancer cell lines
Tested for in vitro cytotoxic activity against CNS U251 human cancer cell lines
[PMID: 12161121]
U-251 GI50
100 3
Compound: 1; Try
Growth inhibition of human U-251 cells assessed as reduction in cell viability
Growth inhibition of human U-251 cells assessed as reduction in cell viability
[PMID: 38665827]
U-251 GI50
100 3
Compound: 47
Growth inhibition of human U-251 cells
Growth inhibition of human U-251 cells
[PMID: 36375335]
U-87MG ATCC IC50
0.194 3
Compound: 5a
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
[PMID: 30321802]
U-87MG ATCC IC50
5 3
Compound: 5a
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
[PMID: 27475108]
U-937 IC50
3.1 6
Compound: 47
Cytotoxicity against human U-937 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
Cytotoxicity against human U-937 cells assessed reduction in cell growth incubated for 48 hrs by MTT assay
[PMID: 36375335]
Vero IC50
> 100 6
Compound: 2
Cytotoxicity against African green monkey Vero cells by CellTiter 96 aqueous nonradioactive cell proliferation assay
Cytotoxicity against African green monkey Vero cells by CellTiter 96 aqueous nonradioactive cell proliferation assay
[PMID: 30295480]
Vero IC50
> 8 6
Compound: 1a, Tryptanthrin
Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
[PMID: 23360475]
WEHI3B IC50
1.5 3
Compound: 1; Try
Antiproliferative activity against mouse WEHI3B cells assessed as inhibition of cell growth measured after 48 hrs
Antiproliferative activity against mouse WEHI3B cells assessed as inhibition of cell growth measured after 48 hrs
[PMID: 38665827]
In Vitro

Tryptanthrin (0-60 μM; 24, 48 and 72 h) inhibits the proliferation and colony formation of MCF-7 cells[1].
Tryptanthrin (6.25-25 μM; 48 h; MCF-7 cells) reverses EMT-associated E-cadherin, MMP-2 and Snail[1].
Tryptanthrin (0-30 μM; 15 min; MCF-7 cells) reduces Leukotriene (LT)-formation in human neutrophils with an IC50 value of 0.6 μM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tryptanthrin Related Antibodies

Cell Viability Assay[1]

Cell Line: MCF-7 cells
Concentration: 0-60 μM
Incubation Time: 24, 48 and 72 hours
Result: Increased the inhibition rates of MCF-7 cells in a dose- and time- dependent manner.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 6.25, 12.5, and 25 μM
Incubation Time: 48 hours
Result: Increased the E-cadherin protein levels and markedly upregulated the protein expression levels of MMP-2 and Snail in MCF-7 cells induced by TGF-β1.
In Vivo

Tryptanthrin (25-100 mg/kg; i.g.; daily, for 13 d; Female Bal b/c mice with 4T1 xenograft) inhibits tumor growth and regulates IL-2, IL-6, IL-10, IL-12 and TNF-α levels in tumor-bearing mice[1].
Tryptanthrin (10 mg/kg; p.o.; male Wistar Han rats) inhibits LTB4 formation in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Bal b/c mice with 4T1 xenograft[1]
Dosage: 25, 50, and 100 mg/kg
Administration: Oral gavage; daily, for 13 days
Result: Inhibited tumor growth in a dose-dependent manner.
Animal Model: Male Wistar Han rats (220–230 g)[2]
Dosage: 10 mg/kg
Administration: Oral administration; once
Result: Reduced LTB4 pleural levels by 46%.
Reduced PGE2 levels (by 42%), exudate volume (by 80%) and the number of infiltrating cells (by 41%).
Molecular Weight

248.24

Formula

C15H8N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC=CC=C2N3C(C4=CC=CC=C4N=C13)=O
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 7.14 mg/mL (28.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0284 mL 20.1418 mL 40.2836 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 0.71 mg/mL (2.86 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.71 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.1 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 0.67 mg/mL (2.70 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 0.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.83%

SDS (393 KB)

COA (255 KB) HNMR (247 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0284 mL 20.1418 mL 40.2836 mL 100.7090 mL
5 mM 0.8057 mL 4.0284 mL 8.0567 mL 20.1418 mL
10 mM 0.4028 mL 2.0142 mL 4.0284 mL 10.0709 mL
15 mM 0.2686 mL 1.3428 mL 2.6856 mL 6.7139 mL
20 mM 0.2014 mL 1.0071 mL 2.0142 mL 5.0354 mL
25 mM 0.1611 mL 0.8057 mL 1.6113 mL 4.0284 mL
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Tryptanthrin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tryptanthrin13220-57-0Leukotriene ReceptorNO SynthaseNF-κBCOXTNF ReceptorInterleukin RelatedNitric oxide synthasesNOSNuclear factor-κBNuclear factor-kappaBCyclooxygenaseTumor Necrosis Factor ReceptorTNFRILindole quinazolineindigo-bearing plantsLeukotriene biosynthesisanticancerMCF-7 cellsInhibitorinhibitorinhibit

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