Lactate Dehydrogenase Inhibitor

PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity.

RS6212 is a specific LDH (lactate dehydrogenase) inhibitor with an IC₅₀ value of 12.03 μM . RS6212 inhibits tumor growth and exhibits potent anticancer activity in multiple cancer cell lines.

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 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model.

LM-021 is a coumarin-chalcone derivative with anti-aggregatory, antioxidant, neuroprotective and anti-inflammatory properties which suppresses nitric oxide (NO), IL-1β, IL-6, TNF-α production, CD68 antigen (CD68) and histocompatibility-2 (MHCII) expression. LM-021 also attenuates the increase of caspase 1 activity, lactate dehydrogenase release and ROS level. LM-021 can be used for neurological research.

ddhCTP trisodium solution (100 mM ± 3 mM) is an endogenously produced pyrimidine base analog with a K_d of 17.0 nM for LLDH and an IC₅₀ of 55.8 μM for GAPDH. By inhibiting key metabolic enzymes such as GAPDH, ddhCTP trisodium reduces glycolytic flux and shifts metabolic flow toward the pentose phosphate pathway, thereby regulating the redox balance of cells. As a competitive CTP analog, ddhCTP trisodium terminates RNA synthesis by flavivirus RdRps and SARS-CoV-2 RdRp, and inhibits Zika virus replication in vivo. ddhCTP trisodium can be used in studies related to viral infections, COVID-19 and Zika virus infections.

NCATS-SM1441 (compound 52) is a lactate dehydrogenase (LDH) inhibitor (IC₅₀=40 nM). By inhibiting the activity of LDH, NCATS-SM1441 is able to reduce the production of lactic acid in cancer cells, helping to slow or stop the proliferation of cancer cells. NCATS-SM1441 can be used to study cancer metabolism.

WQQ-345 is an orally active BCAT1 inhibitor with an IC₅₀ values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer.

FuBIG is an iminoguanidine derivative with neuroprotective effects. FuBIGL inhibits L-LDH activation and reduces lactate production. FuBIGL exerts protective effects on inflammatory nerve cells, upregulates the expressions of AMPK, pAMPK and FOXO3, and activates the AMPK pathway in cells. FuBIG exerts anti-inflammatory effects by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10. FuBIG maintains mitochondrial membrane potential, alleviates mitochondrial dysfunction, reduces ROS production, and relieves oxidative stress. FuBIG upregulates Bcl-2, downregulates Bax and Caspase-3, and inhibits cell apoptosis (apoptosis). FuBIG improves metabolic disorders in diabetic mice, decreases the levels of LDL-C, ALT and AST, and increases HDL-C level simultaneously. FuBIG can be used in the research of diabetic neuroinflammation.

NCATS-SM1440 is a glycolysis inhibitor and metabolic regulator that targets LDHA and LDHB (IC₅₀=0.06 μM and 0.03 μM, respectively). Upon binding to LDHA, NCATS-SM1440 blocks the glycolysis pathway and reduces lactate production. NCATS-SM1440 drives the shift of pyruvate metabolism toward mitochondrial metabolism, effectively disrupting the dependence of cancer cells on aerobic glycolysis. NCATS-SM1440 can be widely used in research related to cancer, Ewing's sarcoma, and other related conditions.

LDHA-IN-5 is a novel, potent, dual GO/LDHA inhibitor for primary hyperoxaluria.

Anticancer agent 121, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research.

LDH-IN-3 (compound E38) is an inhibitor of LDH, promising protective agent for ischemic nerve damage in the eye and brain. LDH-IN-3 acts its function via HO-1/SIRT1 pathway..

Bisadinrone A is a sesquiterpene found in Curcuma longa. Bisadinrone A can inhibit LDH release and shows significant anti-myocardial ischemia-reperfusion injury activity. Bisadinrone A can be used for the research of cardiovascular disease, such as ischemic heart disease.

Linoleylanilide (Linoleic acid anilide) is a Linoleic acid (HY-N0729) derivative. Linoleylanilide slightly inhibits the PMA (HY-18739)-induced expression of CD11b. Linoleylanilide inhibits serum LDH, GOT and GPT activities. Linoleylanilide decreases red cell counts and hemoglobin content.

RIPK1-IN-38 is an orally active RIPK1 inhibitor with an IC₅₀ value of 27 nM. RIPK1-IN-38 can inhibit the phosphorylation of RIPK1 and its downstream signaling molecules RIPK3 and MLKL. RIPK1-IN-38 exhibits anti-necroptotic activity. RIPK1-IN-38 has excellent anti-inflammatory efficacy in both the SIRS model and GVHD model. RIPK1-IN-38 can be used for the research of inflammatory and immune-related diseases.

ZG-2492 is an orally active LDHA inhibitor with an IC₅₀ of 156 nM. ZG-2492 can reduce lactate production and induce cell cycle arrest and apoptosis in pancreatic cancer cells . ZG-2492 has antitumor activity and can be used in the research of tumors such as pancreatic cancer.

Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma.

ddhCTP is an endogenously produced pyrimidine base analog with a K_d of 17.0 nM for LLDH and an IC₅₀ of 55.8 μM for GAPDH. By inhibiting key metabolic enzymes such as GAPDH, ddhCTP reduces glycolytic flux and shifts metabolic flow toward the pentose phosphate pathway, thereby regulating the redox balance of cells. As a competitive CTP analog, ddhCTP terminates RNA synthesis by flavivirus RdRps and SARS-CoV-2 RdRp, and inhibits Zika virus replication in vivo. ddhCTP can be used in studies related to viral infections, COVID-19 and Zika virus infections.

AK-135 hydrochloride is a Menadione (HY-B0332) derivative. AK-135 hydrochloride restores the electron flow in defective respiratory chain systems. AK-135 hydrochloride decreases LDH release, increases the amount of ATP. AK-135 hydrochloride has a protective effect against myocardial injury.

Linalyl acetate-d₆ is deuterated labeled Linalyl acetate (HY-N6948). Linalyl acetate is the principal components of many plant essential oils. Linalyl acetate exhibits anti-anxiety, anti-inflammatory, anti-diabetic, anti-stress, and cardiovascular-regulatory effects. Linalyl acetate is orally active.