1. Metabolic Enzyme/Protease
  2. Lactate Dehydrogenase
  3. 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.

LDHA-IN-1

LDHA-IN-1 Chemical Structure

CAS No. : 1269802-68-7

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Description

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[1].

IC50 & Target[1]

hLDHA

8.9 μM (Ki)

hLDHA

4.7 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
10.8 μM
Compound: 1j
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]
In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: multiple human cancer cell lines, primary pancreatic cancer cultures, immortalized normal cell lines
Concentration: 1-100 μM
Incubation Time: 48 h
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.

Cell Proliferation Assay[1]

Cell Line: LPC006 primary pancreatic cancer cells
Concentration: 1-100 μM
Incubation Time: 48 h
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).
Molecular Weight

321.26

Formula

C16H10F3NO3

CAS No.
SMILES

O=C(O)C1=CC=2C(=CC(=CC2C(F)(F)F)C=3C=CC=CC3)N1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
LDHA-IN-1
Cat. No.:
HY-16964
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