LDHA-IN-1
LDHA-IN-1 is a selective, competitive LDH-A inhibitor, with Ki values of 8.9 μM (NADH assay) and 4.7 μM (Pyruvate assay) against hLDH-A. LDHA-IN-1 inhibits cancer cell proliferation under hypoxic conditions. LDHA-IN-1 can be used in the research of ovarian cancer, colorectal cancer, mesothelioma and pancreatic cancer.
For research use only. We do not sell to patients.
- CAS No.: 1269802-68-7
- Formula: C16H10F3NO3
- Molecular Weight:321.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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hLDHA 8.9 μM (Ki) |
hLDHA 4.7 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
10.8 μM
Compound: 1j
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Cytotoxicity against human A2780 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human A2780 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| ADDP cell line | IC50 |
17 μM
Compound: 1j
|
Cytotoxicity against human ADDP cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human ADDP cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| HS27 | IC50 |
>100 μM
Compound: 1j
|
Cytotoxicity against immortalized human HS27 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against immortalized human HS27 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| MSTO-211H | IC50 |
10.6 μM
Compound: 1j
|
Cytotoxicity against human MSTO-211H cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human MSTO-211H cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| NCI-H2052 | IC50 |
73.2 μM
Compound: 1j
|
Cytotoxicity against human NCI-H2052 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H2052 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| NCI-H2452 | IC50 |
90.2 μM
Compound: 1j
|
Cytotoxicity against human NCI-H2452 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H2452 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| NCI-H28 | IC50 |
11.4 μM
Compound: 1j
|
Cytotoxicity against human NCI-H28 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H28 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
| NCI-H630 | IC50 |
31.5 μM
Compound: 1j
|
Cytotoxicity against human NCI-H630 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H630 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 21332213] |
LDHA-IN-1 (Compound 1j) is a potent inhibitor that acts on purified hLDH-A, with a Ki value of 8.9 μM against NADH and 4.7 μM against pyruvate, while it exhibits only weak inhibitory activity against LDH-B[1].
LDHA-IN-1 (500 μM; 6-12 h) potently inhibits the conversion of glucose to lactate in HeLa cervical cancer cells, reducing the lactate/glucose peak ratio to <0.01 after 12 h of incubation[1].
LDHA-IN-1 (1-100 μM; 48 h) inhibits the proliferation of various cancer cell lines and primary pancreatic cancer cultures under normoxic conditions, with an IC50 range of 10.8 μM to 90.2 μM, and shows no cytotoxicity towards immortalized normal cell lines at concentrations up to 100 μM[1].
LDHA-IN-1 (1-100 μM; 48 h) shows significantly enhanced inhibitory potency against primary pancreatic cancer cells LPC006 under hypoxic conditions, with an IC50 of 0.90 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:multiple human cancer cell lines, primary pancreatic cancer cultures, immortalized normal cell lines
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Concentration:1-100 μM
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Incubation Time:48 h
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Result:Exhibited normoxic IC50 values ranging from 10.8 μM (A2780/cOHP ovarian cancer cells) to 90.2 μM (NIH-H2452 mesothelioma cells) across cancer cell lines.
Showed IC50 values ranging from 13.5 μM (LPC067) to 48.8 μM (LPC028) in primary pancreatic cancer cultures.
Caused no growth inhibition at 100 μM in immortalized normal hTERT-HPNE pancreatic duct cells or Hs27 skin fibroblasts.
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Cell Line:LPC006 primary pancreatic cancer cells
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Concentration:1-100 μM
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Incubation Time:48 h
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Result:Had an IC50 of 0.90 μM under hypoxic conditions, which is significantly lower than its normoxic IC50 of 16.3 μM (P < 0.05).
Chemical Information
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CAS No. 1269802-68-7
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Molecular Weight 321.26
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Formula C16H10F3NO3
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SMILES
O=C(O)C1=CC=2C(=CC(=CC2C(F)(F)F)C=3C=CC=CC3)N1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)