1. Metabolic Enzyme/Protease Apoptosis
  2. Lactate Dehydrogenase Apoptosis
  3. NHI-2

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S/G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppress tumor growth in mice.

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NHI-2 Chemical Structure

NHI-2 Chemical Structure

CAS No. : 1269802-97-2

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Based on 1 publication(s) in Google Scholar

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Description

NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S/G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppress tumor growth in mice[1][2].

In Vitro

NHI-2 (50-200 μM, 8 h) inhibits lactate production in HeLa cells[1].
NHI-2 (12-40 μM, 72 h) inhibits proliferation in B78 cells[2].
NHI-2 (0.1-100 μM, 48 h) has an EC50 of 32 μM against B78 cells[2].
NHI-2 (40 μM, 24 h) increases cell apoptosis when combined with either 30 or 60 mM Oxamate (Oxa) (HY-W013032A)[2].
NHI-2 (40 μM, 24 h) induces cell cycle arrest at S/G2 phases[2].
NHI-2 affects extracellular acidification rate (ECAR) (12-26 μM, 80 min) and ATP (18 μM, 24 h) production, and has a synergistic effect with Oxa[2].

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

Cell Viability Assay[2]

Cell Line: B78-D14 melanoma cells
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: The EC50 values of 32 μM.

Cell Proliferation Assay[2]

Cell Line: B78-D14 melanoma cells
Concentration: 12, 18, 26, 40, μM
Incubation Time: 72 h
Result: Exhibited no effect on B78 cell proliferation at lower concentrations. but decreased cell proliferation at concentrations beginning from 26 μM.

Apoptosis Analysis[2]

Cell Line: B78-D14 melanoma cells
Concentration: 40 μM
Incubation Time: 24 h
Result: Increased cell apoptosis when combined with either 30 or 60 mM Oxa.

Cell Cycle Analysis[2]

Cell Line: B78-D14 melanoma cells
Concentration: 40 μM
Incubation Time: 24 h
Result: Led to an increased cell population in the S and G2 phases.
In Vivo

NHI-2 (0.9 mg/kg; Intra-tumoral; once daily for 15 days) can suppress tumor volume when combined with immune checkpoint inhibitors (ICIs) in murine B78 melanoma tumor model[2].

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

Animal Model: C57BL/6 female mice (6-8 weeks) were intradermally implanted with B78 syngeneic melanoma cells[2]
Dosage: 0.9 mg/kg
Administration: Intra-tumoral (IT) via percutaneous needle puncture; once daily for 15 days
Result: Suppressed tumor volume when combined with checkpoint inhibitors (ICIs).
Molecular Weight

335.28

Formula

C17H12F3NO3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ON1C2=CC(C3=CC=CC=C3)=CC(C(F)(F)F)=C2C=C1C(OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (74.56 mM; Need ultrasonic and warming; 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 2.9826 mL 14.9129 mL 29.8258 mL
5 mM 0.5965 mL 2.9826 mL 5.9652 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.30%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9826 mL 14.9129 mL 29.8258 mL 74.5645 mL
5 mM 0.5965 mL 2.9826 mL 5.9652 mL 14.9129 mL
10 mM 0.2983 mL 1.4913 mL 2.9826 mL 7.4565 mL
15 mM 0.1988 mL 0.9942 mL 1.9884 mL 4.9710 mL
20 mM 0.1491 mL 0.7456 mL 1.4913 mL 3.7282 mL
25 mM 0.1193 mL 0.5965 mL 1.1930 mL 2.9826 mL
30 mM 0.0994 mL 0.4971 mL 0.9942 mL 2.4855 mL
40 mM 0.0746 mL 0.3728 mL 0.7456 mL 1.8641 mL
50 mM 0.0597 mL 0.2983 mL 0.5965 mL 1.4913 mL
60 mM 0.0497 mL 0.2485 mL 0.4971 mL 1.2427 mL
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  • 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.

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NHI-2
Cat. No.:
HY-124309
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