IκB/IKK
Inhibitory Selectivity
Isoform-specific Inhibitors
IκB/IKK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1274 |
BX-795BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. |
Induction of basal p62 Ser403 phosphorylation in ULK1/2-deficient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
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| S2913 |
BAY 11-7082BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells. |
Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
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| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in vitro with IC50 of 50 nM. |
Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
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| S2824 |
TPCA-1TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis. |
AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies. |
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| S2864 |
IMD 0354IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. |
(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, **P < 0.01 and ***P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
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| S6386New |
MRT67307MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells. |
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| S1321New |
Urolithin BUrolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. |
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| S8044 |
BMS-345541BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively. |
(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. *, p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. *, p<0.05.
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| S4907 |
SC-514SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases. |
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| S7352 |
Bay 11-7085BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10-7mol/L salusin-β treatment alone.
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| S0949 |
Cucurbitacin IIbCucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis. |
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| S7851 |
AZD3264AZD3264 is a novel IKK2 inhibitor. |
(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
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| S7697 |
LY2409881LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. |
A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
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| S7948 |
MRT67307 HClMRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy. |
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| S9417 |
HomoplantagininHomoplantaginin (Hispidulin-7-glucoside), a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation. |
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| S0425 |
TBK1/IKKε-IN-2TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. |
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| S8935 |
BAY-985BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM). |
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| S8922 |
TBK1/IKKε-IN-1(compound 1)TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. |
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| S6714 |
INH14INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively. |
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| S3298 |
Caulophylline (N-Methylcytisine)Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation. |
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| S9184 |
Forsythoside BForsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB. |
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| S3168New |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
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| S7441 |
WS3WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
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| S7442 |
WS6WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1274 |
BX-795BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 modulates autophagy via inhibiting ULK1. |
Induction of basal p62 Ser403 phosphorylation in ULK1/2-deficient MEF was suppressed by BX-795, an inhibitor of TBK1. WT ( Ulk1 +/+/Ulk2 +/+) and Ulk1 -/- /Ulk2 -/-(KO) MEF were treated with NaCl/Pi (Con) or 10 uM BX-795 for 6 h, and subjected to immunoblotting with indicated antibodies.
|
|
| S2913 |
BAY 11-7082BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells. |
Immunofluorescence images of Ishikawa cells showing the increase in the nuclear colocalization of ERa (red) and p65 (green) after E2 incubation. Nuclear colocalization is yellow. Treatment with ICI 182,780, PDTC or Bay inhibited the nuclear localization of both ERa and p65. Blue, DAPI-stained nuclei. All pictures were obtained the same day using the same microscope settings. Original magnification 3200, bar =50 um. Arrows, cytoplasmic ERa and p65 staining. ICI, ICI 182,780; Bay, Bay 11-7082.
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| S2882 |
IKK-16 (IKK Inhibitor VII)IKK-16 (IKK Inhibitor VII) is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM in cell-free assays, respectively. IKK-16 also inhibits LRRK2 Ser935 phosphorylation in cells and LRRK2 kinase activity in vitro with IC50 of 50 nM. |
Reduction in IFN-g production in TcREG by IKK-16 coincides with decrease in T-bet and Eomes expression levels. Flow cytometry plots showing cellular analysis for T-bet and Eomes in CD45+CD3+CD8+ population.
|
|
| S2824 |
TPCA-1TPCA-1 (GW683965) is an inhibitor of IKK-2 with IC50 of 17.9 nM in a cell-free assay, inhibits NF-κB pathway, exhibits 22-fold selectivity over IKK-1. TPCA-1 is also an inhibitor of STAT3 and enhances apoptosis. |
AGS cells were treated with cwith IL-1β in the presence of the IKK inhibitor TPCA-1, the p38 MAPK inhibitor BIX02188 and the JNK inhibitor SP600125. Cell lysates were obtained 24 h after IL-1β treatment and immunoblotted with PTEN antibodies. |
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| S2864 |
IMD 0354IMD-0354 (IKK2 Inhibitor V) is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway. |
(B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, **P < 0.01 and ***P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.
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| S6386New |
MRT67307MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells. |
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| S1321New |
Urolithin BUrolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. |
||
| S8044 |
BMS-345541BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM in cell-free assays, respectively. |
(E) After transfection with control or catalase siRNAs for 24 h, A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine for an additional 48 h. Cell viability was then assessed. *, p<0.05. (F) A375 and G361 cells were treated with vehicle or 2.5 µM BMS-345541, 20 µM PS-1145 and/or 50 µM of fotemustine, in the presence or absence of catalase inhibitor 3-Amino-1,2,4-triazole (ATZ, 50 µM) for 48 h. Cell viability was then assessed. *, p<0.05.
|
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| S4907 |
SC-514SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases. |
||
| S7352 |
Bay 11-7085BAY 11-7085 (Bay 11-7083) is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM. |
VSMCs were pretreated with BAY 11-7085 (BAY, 10μmol/L) for 1h and further treated with or without 10-7mol/L salusin-β for 30min. A, Cytoplasmic extracts (Cy) were obtained and the phosphorylated IκBα, IκBα and HDCA3 protein levels were measured by western blot analysis. B, nuclear extracts (Nu) were obtained and the nuclear p50, p65 and HDAC3 protein levels were measured by western blot analysis. Data are expressed as means ± SD (n=3). *P< 0.05 versus the control with no treatment; #P< 0.05 versus 10-7mol/L salusin-β treatment alone.
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| S0949 |
Cucurbitacin IIbCucurbitacin IIb (CuIIb, Dihydrocucurbitacin F, 25-deacetyl hemslecin A) inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB, blocks nuclear translocation of NF-κB and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb exhibits anti-inflammatory activity and induces apoptosis. Cucurbitacin IIb is isolated from Hemsleya amabilis. |
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| S7851 |
AZD3264AZD3264 is a novel IKK2 inhibitor. |
(C) G361 cells were loaded with DCF (ROS probe) and further stimulated with vehicle or indicated IKKβ inhibitors for 3 h. Fluorescence was measured using a fluorescence microplate reader. *, p<0.05 versus control.
|
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| S7697 |
LY2409881LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. |
A549 cells were treated with NF-kB inhibitor LY2409881 (30 nM) for 2 h, followed by western blot analysis of p-NF-kB.
|
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| S7948 |
MRT67307 HClMRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively. MRT67307 potently inhibits ULK1 and ULK2 and blocks autophagy. |
|
|
| S9417 |
HomoplantagininHomoplantaginin (Hispidulin-7-glucoside), a main flavonoid from a traditional Chinese medicine Salvia plebeia, has anti-inflammatory and anti-oxidant properties. Homoplantaginin inhibits TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation. |
||
| S0425 |
TBK1/IKKε-IN-2TBK1/IKKε-IN-2 (Ikk epsilon-in-1, IKKε-IN-1, MDK10496) is a dual inhibitor of TBK1 and IKKε. |
||
| S8935 |
BAY-985BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. BAY-985 shows high potency toward TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε(IC50 = 2 nM), as well as high potency in the mechanistic pIRF3 assay (IC50 = 74 nM), and an antiproliferative effect on SK-MEL-2 cells (IC50 = 900 nM). |
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| S8922 |
TBK1/IKKε-IN-1(compound 1)TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. |
||
| S6714 |
INH14INH14 is an inhibitor of TLR2-mediated NF-kB activation with IC50 values of 8.975 μM and 3.598 μM for IKKα and IKKβ, respectively. |
||
| S3298 |
Caulophylline (N-Methylcytisine)Caulophylline (N-Methylcytisine, Caulophyllin, NMC) is a tricyclic quinolizidine alkaloid with anti-inflammatory activities. Caulophylline binds to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia with Kd of 50 nM. Caulophylline significantly reduces myeloperoxidase (MPO) activity, blocks the activation of NF-κB by inhibiting IκB and IKK phosphorylation. |
||
| S9184 |
Forsythoside BForsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant. Forsythoside B has potent neuroprotective effects and has anti-inflammation, antioxidant, and antisepsis properties. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3168New |
cis-Resveratrolcis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis. Resveratrol also inhibits a wide spectrum of targets including 5-lipoxygenase (LOX), cyclooxygenase (COX), IKKβ, DNA polymerases α and δ with IC50 of 2.7 μM, <1 μM, 1 μM, 3.3 μM and 5 μM, respectively. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7441 |
WS3WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
||
| S7442 |
WS6WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
