S1950 |
Metformin HCl
|
Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
-
Nat Commun, 2024, 15(1):1785
-
J Clin Invest, 2024, e175023
-
EBioMedicine, 2024, 102:105090
|
|
S4701 |
2-DG (2-Deoxy-D-glucose)
|
2-DG (2-Deoxy-D-glucose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression. |
-
Nat Commun, 2025, 16(1):212
-
Adv Sci (Weinh), 2025, 12(8):e2411943
-
PeerJ, 2025, 13:e18887
|
|
S2610 |
Lonidamine
|
Lonidamine is an orally administered small molecule hexokinase inactivator. |
-
Cancer Lett, 2024, 589:216824
-
Mol Oncol, 2023, 17(9):1821-1843
-
Mol Oncol, 2023, 17(9):1821-1843
|
|
S5426 |
Bromopyruvic acid (3-BP)
|
Bromopyruvic acid (3-BP) is a hexokinase II inhibitor with Ki of 2.4 mM for glycolysis/hexokinase inhibition. It is inhibitor of tumour cell energy metabolism and chemopotentiator of platinum drugs. |
-
iScience, 2024, 27(3):109246
-
Cancer Sci, 2024, 10.1111/cas.16204
-
EMBO Rep, 2023, e56325.
|
|
S2035 |
Epalrestat
|
Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM. |
-
Cell Rep Med, 2023, 4(6):101056
-
Cell Rep Med, 2023, 4(6):101056
-
Free Radic Biol Med, 2021, 163:220-233
|
|
S2155 |
LY2608204
|
LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2. |
-
Sci Rep, 2017, 7:44681
-
Nat Commun, 2016, 7:11463
|
|
S1271 |
Acarbose
|
Acarbose(BAY g 5421,Prandase, Precose, Glucobay, Bay-g 5421) is an inhibitor of intestinal alpha-glucosidase, used to treat type 2 diabetes mellitus. |
-
Infect Genet Evol, 2020, 81:104210
|
|
S3300 |
Desoxyrhaponticin
|
Desoxyrhaponticin (DC, DES), a stilbene glycoside from Rheum tanguticum Maxim. ex Balf. (rhubarb) which is a traditional Chinese nutritional food, is a fatty acid synthase (FAS/FASN) inhibitor. Desoxyrhaponticin (DC, DES) is also a competitive inhibitor of glucose uptake with IC50 of 148.3 μM and 30.9 μM in rabbit intestinal membrane vesicles and in rat everted gut sleeves, respectively. Desoxyrhaponticin has apoptotic effect on human cancer cells. |
-
Nat Metab, 2021, 10.1038/s42255-021-00479-4
|
|
S3839 |
1-Deoxynojirimycin
|
1-Deoxynojirimycin (duvoglustat, moranolin) is a potent α-glucosidase inhibitor and most commonly found in mulberry leaves. It has therapeutic potency against diabetes mellitus. |
-
J Biol Chem, 2022, 298(12):102643
|
|
S6921 |
Dorzagliatin
|
Dorzagliatin (HMS-5552, RO-5305552, Sinogliatin) is a dual-acting glucokinase (GK) activator that improves glycaemic control and pancreatic β-cell function in patients with type 2 diabetes. |
-
Proc Natl Acad Sci U S A, 2022, 119(31):e2204407119
|
|
S3918 |
4',7-Dimethoxy-5-Hydroxyflavone
|
4',7-Dimethoxy-5-Hydroxyflavone (4',7-dimethylapigenin, apigenin dimethylether, apigenin 7,4'-dimethyl ether) inhibits α-glucosidase and α-amylase enzymes and enhances 2-NBDG uptake in L6 cells. |
-
Nat Cell Biol, 2022, 24(3):364-372
|
|
S4101 |
Voglibose
|
Voglibose (AO 128) is an N-substituted derivative of valiolamine, excellent inhibitory activity against α-glucosidases and its action against hyperglycemia and various disorders caused by hyperglycemia. |
-
G3 (Bethesda), 2020, 4;10(5):1585-1597
|
|
E4744New |
BI-9787
|
BI-9787 is a potent zwitterion inhibitor of ketohexokinase(KHK) with IC50 values of 12 nM and 12.8 nM for hKHK-A and hKHK-C. It exhibits good metabolic stability in rat hepatocytes and serves as a potent tool compound for in vitro and in vivo studies in rodents. |
|
|
E8270New |
Eleutherol
|
Eleutherol (Allium A) is a naphthalene extracted from the bulb of E. americana and a potent inhibitor of α-glucosidase with an IC50 of >1.00 μM. It also exhibits significant antifungal activity with MIC values between 7.8µg/mL and 250 µg/mL. It can be used in research on antimicrobial infections and diabetes treatment. |
|
|
S3278 |
Kaempferol-3-O-neohesperidoside
|
Kaempferol 3-neohesperidoside (Kaempferol 3-O-neohesperidoside), a flavonoid isolated from the leaf extract of Primula latifolia Lapeyr. and Primula vulgaris Hudson, stimulates glycogen synthesis in rat soleus muscle via PI3K - GSK-3 pathway and MAPK - PP1 pathway. |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
|
|
E1353 |
AZD1656
|
AZD1656 is a potent, selective and orally active activator of glucokinase. AZD1656 has the potential for type 2 diabetes research. |
-
Liver Res-Prc, 2023, Volume 7, Issue 2 Pages 124-135
|
|
S2589 |
Miglitol
|
Miglitol is an oral anti-diabetic drug. |
|
|
E0477 |
N-Caffeoyl O-methyltyramine
|
N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitory activity against α-glucosidase with IC50 of 103.58 μM. |
|
|
S3243 |
Zeaxanthin
|
Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM. |
|
|
E2846 |
FBPase-1 inhibitor-1
|
FBPase-1 inhibitor-1, an allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1), exhibits similar potency (IC50 = 3.4 μM using MG; = 4.0 μM in the coupled format) in these two distinct assays of FBPase-1 activity. |
|
|
S0553 |
Butyl isobutyl phthalate
|
Butyl isobutyl phthalate (BIP), isolated from the rhizoid of Laminaria japonica, is a non-competitive inhibitor of α-glucosidase with IC50 of 38 μM. Butyl isobutyl phthalate displays a significant hypoglycemic effect and has the potential for diabetes treatment. |
|
|
S3527 |
AM2394
|
AM-2394 is a structurally distinct glucokinase activator (GKA), activates glucokinase (GK) with an EC50 of 60 nM. |
|
|
S0808 |
Ketohexokinase inhibitor 1
|
Ketohexokinase inhibitor 1 (PF-06835919, MDK1846) is a potent inhibitor of ketohexokinase (KHK) with IC50 of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively. |
|
|
S9378 |
4',5-Dihydroxyflavone
|
4',5-Dihydroxyflavone inhibits soybean LOX-1 and yeast α-glucosidase. |
|
|
S3796 |
Rebaudioside A
|
Rebaudioside A (Stevia Extract, Reb A, Glycoside A3, Stevioside A3), an natural sweetening ingredient extracted from the stevia leaf, is used in powder or liquid form to heighten sweetening intensity and improve taste. |
|
|
S2949 |
KPLH1130
|
KPLH1130 is a specific inhibitor of pyruvate dehydrogenase kinase (PDK) that blocks macrophage polarization and attenuates proinflammatory responses. |
|
|
S4793 |
Cedryl acetate
|
Cedryl Acetate (Cedrol acetate, Cedranyl acetate), an acetylated from cedarwood oil, has been applied to chemistry for its properties as a chiral and cell signaling reagent with antifungal and immunotoxicity functions. Cedryl acetate exhibits α-glucosidase inhibitory activity. |
|
|
E4014 |
4-Nitrophenyl alpha-D-glucopyranoside
|
4-Nitrophenyl alpha-D-glucopyranoside is a chromogenic substrate in the α-glucosidase inhibition assay. |
|
|
S5426 |
Bromopyruvic acid (3-BP)
|
Bromopyruvic acid (3-BP) is a hexokinase II inhibitor with Ki of 2.4 mM for glycolysis/hexokinase inhibition. It is inhibitor of tumour cell energy metabolism and chemopotentiator of platinum drugs. |
- iScience, 2024, 27(3):109246
- Cancer Sci, 2024, 10.1111/cas.16204
- EMBO Rep, 2023, e56325.
|
|
S3300 |
Desoxyrhaponticin
|
Desoxyrhaponticin (DC, DES), a stilbene glycoside from Rheum tanguticum Maxim. ex Balf. (rhubarb) which is a traditional Chinese nutritional food, is a fatty acid synthase (FAS/FASN) inhibitor. Desoxyrhaponticin (DC, DES) is also a competitive inhibitor of glucose uptake with IC50 of 148.3 μM and 30.9 μM in rabbit intestinal membrane vesicles and in rat everted gut sleeves, respectively. Desoxyrhaponticin has apoptotic effect on human cancer cells. |
- Nat Metab, 2021, 10.1038/s42255-021-00479-4
|
|
S3918 |
4',7-Dimethoxy-5-Hydroxyflavone
|
4',7-Dimethoxy-5-Hydroxyflavone (4',7-dimethylapigenin, apigenin dimethylether, apigenin 7,4'-dimethyl ether) inhibits α-glucosidase and α-amylase enzymes and enhances 2-NBDG uptake in L6 cells. |
- Nat Cell Biol, 2022, 24(3):364-372
|
|
S4101 |
Voglibose
|
Voglibose (AO 128) is an N-substituted derivative of valiolamine, excellent inhibitory activity against α-glucosidases and its action against hyperglycemia and various disorders caused by hyperglycemia. |
- G3 (Bethesda), 2020, 4;10(5):1585-1597
|
|
E4744New |
BI-9787
|
BI-9787 is a potent zwitterion inhibitor of ketohexokinase(KHK) with IC50 values of 12 nM and 12.8 nM for hKHK-A and hKHK-C. It exhibits good metabolic stability in rat hepatocytes and serves as a potent tool compound for in vitro and in vivo studies in rodents. |
|
|
E8270New |
Eleutherol
|
Eleutherol (Allium A) is a naphthalene extracted from the bulb of E. americana and a potent inhibitor of α-glucosidase with an IC50 of >1.00 μM. It also exhibits significant antifungal activity with MIC values between 7.8µg/mL and 250 µg/mL. It can be used in research on antimicrobial infections and diabetes treatment. |
|
|
S3245 |
Nodakenetin
|
Nodakenetin (NANI), a plant-derived coumarin isolated from Angelica decursiva, inhibits α-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and β-site amyloid precursor protein cleaving enzyme 1 (BACE1). Nodakenetin alters the protein expression of Bax and Bcl-2, and prompts mitochondrial apoptosis. Nodakenetin exhibits anti-tumor activity. |
|
|
S2589 |
Miglitol
|
Miglitol is an oral anti-diabetic drug. |
|
|
E0477 |
N-Caffeoyl O-methyltyramine
|
N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitory activity against α-glucosidase with IC50 of 103.58 μM. |
|
|
S3243 |
Zeaxanthin
|
Zeaxanthin, the carotenoid alcohol participates in the xanthophyll cycle, activates the extrinsic apoptosis pathway which induces apoptosis on uveal melanoma cells with IC50 value 40.8 µM. |
|
|
E2846 |
FBPase-1 inhibitor-1
|
FBPase-1 inhibitor-1, an allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1), exhibits similar potency (IC50 = 3.4 μM using MG; = 4.0 μM in the coupled format) in these two distinct assays of FBPase-1 activity. |
|
|
S0553 |
Butyl isobutyl phthalate
|
Butyl isobutyl phthalate (BIP), isolated from the rhizoid of Laminaria japonica, is a non-competitive inhibitor of α-glucosidase with IC50 of 38 μM. Butyl isobutyl phthalate displays a significant hypoglycemic effect and has the potential for diabetes treatment. |
|
|
S0808 |
Ketohexokinase inhibitor 1
|
Ketohexokinase inhibitor 1 (PF-06835919, MDK1846) is a potent inhibitor of ketohexokinase (KHK) with IC50 of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively. |
|
|
S9378 |
4',5-Dihydroxyflavone
|
4',5-Dihydroxyflavone inhibits soybean LOX-1 and yeast α-glucosidase. |
|
|
S3796 |
Rebaudioside A
|
Rebaudioside A (Stevia Extract, Reb A, Glycoside A3, Stevioside A3), an natural sweetening ingredient extracted from the stevia leaf, is used in powder or liquid form to heighten sweetening intensity and improve taste. |
|
|
S2949 |
KPLH1130
|
KPLH1130 is a specific inhibitor of pyruvate dehydrogenase kinase (PDK) that blocks macrophage polarization and attenuates proinflammatory responses. |
|
|
S4793 |
Cedryl acetate
|
Cedryl Acetate (Cedrol acetate, Cedranyl acetate), an acetylated from cedarwood oil, has been applied to chemistry for its properties as a chiral and cell signaling reagent with antifungal and immunotoxicity functions. Cedryl acetate exhibits α-glucosidase inhibitory activity. |
|
|
S4701 |
2-DG (2-Deoxy-D-glucose)
|
2-DG (2-Deoxy-D-glucose), an analog of glucose, is a glycolytic inhibitor with antiviral activity. 2-Deoxy-D-glucose induces apoptosis and inhibits Herpes Simplex Virus type-1 (HSV-1) receptor expression. |
- Nat Commun, 2025, 16(1):212
- Adv Sci (Weinh), 2025, 12(8):e2411943
- PeerJ, 2025, 13:e18887
|
|
S2610 |
Lonidamine
|
Lonidamine is an orally administered small molecule hexokinase inactivator. |
- Cancer Lett, 2024, 589:216824
- Mol Oncol, 2023, 17(9):1821-1843
- Mol Oncol, 2023, 17(9):1821-1843
|
|
S2035 |
Epalrestat
|
Epalrestat is an aldose reductase inhibitor with IC50 of 72 nM. |
- Cell Rep Med, 2023, 4(6):101056
- Cell Rep Med, 2023, 4(6):101056
- Free Radic Biol Med, 2021, 163:220-233
|
|
S2155 |
LY2608204
|
LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2. |
- Sci Rep, 2017, 7:44681
- Nat Commun, 2016, 7:11463
|
|
S3839 |
1-Deoxynojirimycin
|
1-Deoxynojirimycin (duvoglustat, moranolin) is a potent α-glucosidase inhibitor and most commonly found in mulberry leaves. It has therapeutic potency against diabetes mellitus. |
- J Biol Chem, 2022, 298(12):102643
|
|
S3278 |
Kaempferol-3-O-neohesperidoside
|
Kaempferol 3-neohesperidoside (Kaempferol 3-O-neohesperidoside), a flavonoid isolated from the leaf extract of Primula latifolia Lapeyr. and Primula vulgaris Hudson, stimulates glycogen synthesis in rat soleus muscle via PI3K - GSK-3 pathway and MAPK - PP1 pathway. |
|
|