STAT

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1155 S3I-201 <1 mg/mL 73 mg/mL <1 mg/mL
S1014 Bosutinib (SKI-606) <1 mg/mL 100 mg/mL ''''2 mg/mL
S1491 Fludarabine <1 mg/mL 57 mg/mL '<1 mg/mL
S2796 WP1066 <1 mg/mL 71 mg/mL '<1 mg/mL
S1396 Resveratrol <1 mg/mL 45 mg/mL ''<1 mg/mL
S6784 STAT5-IN-1 <1 mg/mL 20 mg/mL <1 mg/mL
S7024 Stattic <1 mg/mL 42 mg/mL '<1 mg/mL
S2824 TPCA-1 <1 mg/mL 56 mg/mL ''<1 mg/mL
S3030 Niclosamide <1 mg/mL <1 mg/mL <1 mg/mL
S4182 Nifuroxazide <1 mg/mL 55 mg/mL <1 mg/mL
S7337 SH-4-54 <1 mg/mL 100 mg/mL 50 mg/mL
S8685 AS1517499 <1 mg/mL 79 mg/mL 36 mg/mL
S7977 Napabucasin(BBI608) <1 mg/mL 10 mg/mL <1 mg/mL
S2265 Artesunate <1 mg/mL 77 mg/mL 77 mg/mL
S7769 BP-1-102 <1 mg/mL 100 mg/mL <1 mg/mL
S2285 Cryptotanshinone <1 mg/mL 5 mg/mL 1 mg/mL
S7923 SH5-07 (SH-5-07) <1 mg/mL 100 mg/mL 100 mg/mL
S9015 Homoharringtonine -1 mg/mL 100 mg/mL -1 mg/mL
S7951 Ochromycinone (STA-21) <1 mg/mL 21 mg/mL 2 mg/mL
S8561 HJC0152 <1 mg/mL 88 mg/mL <1 mg/mL
S3810 Scutellarin -1 mg/mL 50 mg/mL -1 mg/mL
S8197 APTSTAT3-9R 98 mg/mL <1 mg/mL <1 mg/mL
S8605 C188-9 <1 mg/mL 94 mg/mL 6 mg/mL
S7501 HO-3867 <1 mg/mL 13 mg/mL 6 mg/mL

亜型選択性的な製品

STAT製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1155

S3I-201

S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.

S1014

Bosutinib (SKI-606)

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.

S1491

Fludarabine

Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.

S2796

WP1066

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.

S1396

Resveratrol

Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

S6784

STAT5-IN-1

STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform.

S7024

Stattic

Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.

S2824

TPCA-1

TPCA-1 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.

S3030

Niclosamide

Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).

S4182

Nifuroxazide

Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells.

S7337

SH-4-54

SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.

S8685

AS1517499

AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.

S7977

Napabucasin(BBI608)

Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor.

S2265

Artesunate

Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.

S7769

BP-1-102

BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM.

S2285

Cryptotanshinone

Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5.

S7923

SH5-07 (SH-5-07)

SH5-07 is a robust hydroxamic acid-based STAT3 inhibitor, which induce antitumor cell effects in vitro and antitumor response in vivo against human glioma and breast cancer models.

S9015

Homoharringtonine

Homoharringtonine, a plant alkaloid with antitumor properties, inhibit protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site

S7951

Ochromycinone (STA-21)

Ochromycinone (STA-21) is a selective STAT3 inhibitor.

S8561

HJC0152

HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.

S3810

Scutellarin

Scutellarin, the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities.

S8197

APTSTAT3-9R

APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of APTSTAT3-9R in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets.

S8605

C188-9

C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

S7501

HO-3867

HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1155

S3I-201

S3I-201 shows potent inhibition of STAT3 DNA-binding activity with IC50 of 86 μM in cell-free assays, and low activity towards STAT1 and STAT5.

S1014

Bosutinib (SKI-606)

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.

S1491

Fludarabine

Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.

S2796

WP1066

WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. WP1066 induces apoptosis. Phase 1.

S1396

Resveratrol

Resveratrol has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.

S6784

STAT5-IN-1

STAT5-IN-1 is a potent and selective STAT5 inhibitor with IC50 of 47 μM for STAT5β isoform.

S7024

Stattic

Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.

S2824

TPCA-1

TPCA-1 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.

S3030

Niclosamide

Niclosamide can inhibit DNA replication and inhibit STAT3 with IC50 of 0.7 μM in a cell-free assay. Niclosamide selectively inhibited the phosphorylation of STAT3 and had no obvious inhibition against the activation of other homologues (e.g., STAT1 and STAT5).

S4182

Nifuroxazide

Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells.

S7337

SH-4-54

SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.

S8685

AS1517499

AS1517499 is a novel and potent STAT6 inhibitor with an IC50 value of 21 nM.

S7977

Napabucasin(BBI608)

Napabucasin is an orally available Stat3 and cancer cell stemness inhibitor.

S2265

Artesunate

Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.

S7769

BP-1-102

BP-1-102 is a potent, orally bioavailable and selective STAT3 inhibitor, binds Stat3 with an affinity Kd of 504 nM and blocks Stat3-phospho-tyrosine (pTyr) peptide interactions and Stat3 activation at 4-6.8 μM.

S2285

Cryptotanshinone

Cryptotanshinone is a STAT3 inhibitor with IC50 of 4.6 μM in a cell-free assay, strongly inhibits phosphorylation of STAT3 Tyr705, with a small effect on STAT3 Ser727, but none against STAT1 nor STAT5.

S7923

SH5-07 (SH-5-07)

SH5-07 is a robust hydroxamic acid-based STAT3 inhibitor, which induce antitumor cell effects in vitro and antitumor response in vivo against human glioma and breast cancer models.

S9015

Homoharringtonine

Homoharringtonine, a plant alkaloid with antitumor properties, inhibit protein translation by preventing the initial elongation step of protein synthesis via an interaction with the ribosomal A-site

S7951

Ochromycinone (STA-21)

Ochromycinone (STA-21) is a selective STAT3 inhibitor.

S8561

HJC0152

HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.

S3810

Scutellarin

Scutellarin, the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities.

S8197

APTSTAT3-9R

APTSTAT3-9R is a specific STAT3-binding peptide with addition of a cell-penetrating motif. The treatment of APTSTAT3-9R in various types of cancer cells blocks STAT3 phosphorylation and reduces expression of STAT targets.

S8605

C188-9

C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

S7501

HO-3867

HO-3867, an analog of curcumin, is a selective STAT3 inhibitor that inhibits its phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

Tags: STAT inhibition | STAT signaling pathway | STAT pathway | STAT cancer | STAT signaling | STAT protein | STAT activation | JAK-STAT signaling pathway | STAT3 pathway | STAT3 cancer | STAT3 inhibition | STAT3 activation | STAT phosphorylation | STAT3 protein | STAT1 inhibition | STAT1 pathway | STAT1 activation | STAT1 protein | JAK-STAT mechanism | STAT3 inhibitors in clinical trials | STAT3 inhibitor in vivo | STAT inhibitor review