2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis
  3. Lactate Dehydrogenase Reactive Oxygen Species (ROS) Apoptosis
  4. NCI-006

NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targeting glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model.

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NCI-006

NCI-006 Chemical Structure

CAS No. : 1964516-64-0

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Description

NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targeting glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model[1][2][3][4][5][6][7].

In Vitro

NCI-006 (0-1 μM) inhibits the activity of human LDH (hLDH), and the HEK293T cells isoenzymes 2, 3, 4, 5 and mouse isoenzymes 1, 2, 3, 4, 5, does not inhibit the activity of malate dehydrogenase (MDH) and succinate dehydrogenase (SDH) isolated from human kidney[3].
NCI-006 (0.2-5 μM,2 h) reduces the NAD/NADH ratio in MIA PaCa-2 and HT29 cells, affects lactate secretion in mouse (m) and human (h) red blood cells (RBCs) as well as MIA PaCa-2 and HT29 cells, with EC50s of 1.6, 2.1, 0.37, 0.53 μM [3].
NCI-006(0-10 μM, 0-180 min) reduces the basal extracellular acidification rate (ECAR) in a time-dependent manner at a minimum concentration of 1 μM and inhibits glycolysis at concentrations ≥ 1 μM, and improves basic oxygen consumption rate (OCR) in MIA PaCa-2 cells[3].
NCI-006 (1 μM) combined with IACS-010759 (HY-112037) reduces cell viability in MIA PaCa-2, HCT116, and MKN45 cells[3][6].
NCI-006 (5 μM) reduces OCR, ECAR, sugar ATP production rate, has no change of mito ATP production rate or total ATP production rate, does not increase mitotic ATP production rate, but significantly increases sugar ATP production rate in combination with IACS-010759 (HY-112037) in HCT116 and MKN45 cells[6].
NCI-006 (72 h) inhibits ewing sarcoma cell lines proliferation, with IC50s ranging from 100 nmol/L (TC71 and TC32) to 1 μmol/L (RDES and EW8), has no effect of rhabdomyosarcoma and osteosarcoma, with an IC50 of 1037 nmol/L[7].
NCI-006 dose-dependently inhibits LDH activity in TC71, TC32, EW8 cells, with IC50s approximately 100 nmol/L[7].
NCI-006 (0.1-10 μM, 2 h) inhibits ECAR in TC71 and EW8 cells[7].

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

NCI-006 Related Antibodies
In Vivo

NCI-006 (0-200 mg/kg, p.o./i.v., once) reduces LDH activity at 2 h in female athymic nude mice [3].
NCI-006 (50 mg/kg, p.o./i.v., once; i.v., every other day for 1 week, or for 2 weeks) inhibits tumor LDH activity, resulting in decreased conversion of pyruvate to lactate, with enhanced pyruvate flux to bicarbonate and mitochondrial oxidation, without a detectable increase in transaminase-mediated pyruvate flux to alanine, slows the tumor growth in MIA PaCa-2/HT29 tumor female athymic nude mice[3].
NCI-006 (40 mg/kg, i.v., 2/3 times a week, 1/2 weeks) treatment alone does not inhibit tumor growth, inhibits tumor growth in combination with IACS-010759 (HY-112037) in HCT116 and MKN45 xenografts nude mice[6].
NCI-006 (50 mg/kg, p.o., once or twice daily, 3 weeks) has little change in tumor growth in TC71, TC32, and EW8 xenografts female Fox Chase SCID beige mice[7].

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

Animal Model: Female athymic nude mice (20-25 g)[3]
Dosage: 0 mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg
Administration: p.o., once
Result: Dose-dependent reduced LDH activity at 2 h, but in most cases, recovery to baseline levels by 24 h, 75%-80% of baseline at 24 h, with maximal inhibition maintained at 8 h.
Animal Model: Female athymic nude mice (20-25 g)[3]
Dosage: 0 mg/kg, 10 mg/kg, 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: i.v., once
Result: Dose-dependent reduced LDH activity at 2 h, but in most cases, recovery to baseline levels by 24 h.
Animal Model: MIA PaCa-2 tumor female athymic nude mice (20-25 g)[3]
Dosage: 50 mg/kg
Administration: p.o./i.v., once; i.v., every other day for 1 week (three injections, Monday, Wednesday, and Friday), or for 2 weeks (six injections) with a break of 1 week between cycles.
Result: Inhibits LDH by 80% at intratumoral drug levels of approximately 20 μM.
Dose dependently suppressed the tumor [13C]lactate/[13C]pyruvate ratio, did not affect the [13C]lactate/[13C]pyruvate ratio in MIA PaCa-2 tumors (up to 7 h after drug administration).
Slowed the growth of MIA PaCa-2 xenografts without a marked effect on mouse body weight.
Reduced conversion of [13C]pyruvate to both [13C]lactate and [13C]bicarbonate, more significantly inhibits tumor growth in combination with IACS-010759 (HY-112037).
Animal Model: HT29 tumor female athymic nude mice (20-25 g)[3]
Dosage: 50 mg/kg
Administration: i.v., once
Result: Decreased the [13C]Lac/[13C]Pyr ratio by 74.7%.
More significantly inhibits tumor growth when combined with Metformin(HY-B0627).
Animal Model: HCT116 (5×106) xenografts nude mice (18-24 g, six-week-old female KSN/slc athymic)[6]
Dosage: 40 mg/kg
Administration: i.v., 3 times a week, 1 weeks
Result: Treatment alone did not inhibit tumor growth, inhibited tumor growth and transiently and significantly increased AST, ALT, amylase, lipase, creatinine, and bilirubin levels in combination with IACS-010759 (HY-112037).
Decreased the 13C-L/P ratio, increased ROS levels.
Animal Model: MKN45 xenografts nude mice (18-24 g, six-week-old female KSN/slc athymic)[6]
Dosage: 40 mg/kg
Administration: i.v., 2 times a week, 2 weeks
Result: Treatment alone did not inhibit tumor growth, inhibited tumor growth and transiently and significantly increased AST, ALT, amylase, lipase, creatinine, and bilirubin levels in combination with IACS-010759 (HY-112037).
Decreased the 13C-L/P ratio.
Animal Model: TC71, TC32, and EW8 xenografts female Fox Chase SCID beige mice [7]
Dosage: 50 mg/kg
Administration: p.o., once or twice daily, 3 weeks
Result: Had little change in tumor growth.
Molecular Weight

650.74

Formula

C31H24F2N4O4S3
CAS No.
SMILES

O=C(C1=CSC(N2N=C(C(CC3=CC=C(S(=O)(N)=O)C(F)=C3)=C2CC4CC4)C5=CC(C#CC6=CC=C(C)S6)=C(F)C=C5)=N1)O
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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.

Keywords:

NCI-0061964516-64-0NCI006NCI 006Lactate DehydrogenaseReactive Oxygen Species (ROS)ApoptosisLDHInhibitorapoptosisglycolysisEwing sarcoma modelMKN45 cellsMIA PaCa-2 cellsHCT116 cellsHT29 cellsnude miceinhibitorinhibit

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