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PROTAC CDK8-cyclin C dual degrader
LL-K8-22 is a potent, selective, and durable PROTAC degrader targeting the CDK8–cyclin C complex, with DC₅₀ values of 2.52 μM and 2.64 μM, respectively. It suppresses STAT1 Ser727 phosphorylation and inhibits E2F- and MYC-driven oncogenic transcriptional programs. LL-K8-22 shows potential for use in triple-negative breast cancer (TNBC) research and related therapeutic studies. -
PROTAC STAT3 Degrader
SD-36 is a selective PROTAC degrader of STAT3 that induces potent degradation of STAT3 protein both in vitro and in vivo, with minimal impact on other STAT family members. By suppressing STAT3-driven transcriptional programs, SD-36 inhibits the proliferation of acute myeloid leukemia and anaplastic large-cell lymphoma cells through cell cycle arrest and apoptosis. In xenograft mouse models, SD-36 achieves complete and sustained tumor regression at well-tolerated doses, making it a promising tool for cancer research and targeted therapy development. -
STAT5 Degrader
AK-2292 is a potent and selective degrader of the STAT5 transcription factor, exhibiting a DC50 of 0.10 μM. This compound effectively induces the degradation of STAT5A/B proteins both in vitro and in vivo, demonstrating potential for tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models. Additionally, AK-2292 features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, making it a valuable tool for chemical biology applications. -
STAT3/NF-κB Inhibitor
Triacetylresveratrol is an acetylated analog of Resveratrol that functions as an inhibitor of STAT3 and NF-κB signaling pathways. It effectively reduces the phosphorylation levels of STAT3 and NF-κB in a dose- and time-dependent manner in PANC-1 and BxPC-3 cancer cell lines. Its promising anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
Antihelminthic Agent
Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells. -
PTPN1/PTPN2 Inhibitor
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction. -
STAT3 Inhibitor
Pentadecanoic acid is a saturated fatty acid that serves as an inhibitor of STAT3, a critical transcription factor involved in cellular signaling pathways. Its primary biological activity includes modulation of inflammatory responses and potential anti-cancer effects. This compound is utilized in research applications focused on cancer therapy, inflammation studies, and metabolic regulation. -
STAT3 Inhibitor
STAT3-IN-13 is a potent inhibitor of the STAT3 signaling pathway, specifically targeting the SH2 domain with a binding affinity of 0.46 μM. This compound effectively inhibits the phosphorylation of STAT3 at Y705, subsequently reducing the expression of downstream target genes. In vitro studies demonstrate its ability to induce apoptosis, while in vivo applications show suppression of tumor growth and metastasis. STAT3-IN-13 is a valuable tool for cancer research, particularly in studies focused on the modulation of aberrant STAT3 activity. -
STAT3 Inhibitor
Atiprimod hydrochloride is a potent inhibitor of the signal transducer and activator of transcription 3 (STAT3). It demonstrates significant antitumor, anti-inflammatory, and anti-angiogenic properties by blocking IL-6 and VEGF signaling pathways, inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod effectively induces cell cycle arrest, autophagy, and apoptosis in various cancer cell types, particularly through the activation of the PERK/eIF2α/ATF4/CHOP pathway in breast cancer cells. Its efficacy in tumor xenograft mouse models underscores its potential for investigating therapeutic approaches in conditions such as pituitary adenoma, breast cancer, multiple myeloma, and acute myeloid leukemia (AML). -
STAT3 Inhibitor
Atiprimod dimaleate is a selective inhibitor of the transcription factor STAT3, demonstrating significant antitumor, anti-inflammatory, and anti-angiogenic properties. By disrupting IL-6 and VEGF signaling pathways, it inhibits the phosphorylation of JAK2 and JAK3, effectively blocking the JAK-STAT signaling cascade. Atiprimod dimaleate induces cell cycle arrest, promotes autophagy and apoptosis, and activates the PERK/eIF2α/ATF4/CHOP pathway to trigger ER stress-mediated apoptosis in cancer cells. This reagent is valuable for research related to breast cancer, pituitary adenoma, multiple myeloma, and acute myeloid leukemia (AML), and has shown promising anti-tumor activity in xenograft mouse models. -
STAT1/3 Inhibitor
STAT1/3-IN-1 is a potent inhibitor of STAT1 and STAT3, targeting the phosphorylation and nuclear translocation of these transcription factors. This compound demonstrates significant anti-inflammatory activity by reducing LPS-induced production of pro-inflammatory cytokines such as NO, IL-1β, IL-6, and TNF-α, as well as inflammatory mediators like iNOS and COX-2. STAT1/3-IN-1 exhibits low toxicity in murine models, making it a valuable tool for investigating neuroinflammation and its underlying mechanisms. -
STAT3 Inhibitor
W1131 is a potent inhibitor of signal transducer and activator of transcription 3 (STAT3), which plays a critical role in oncogenic processes. By inducing ferroptosis, W1131 effectively suppresses cancer progression in various models, including gastric cancer subcutaneous xenografts, organoids, and patient-derived xenografts (PDX). Additionally, W1131 enhances chemosensitivity of cancer cells to 5-fluorouracil (5-FU), while modulating cell cycle dynamics, DNA damage response, and oxidative phosphorylation via the IL6-JAK-STAT3 and ferroptosis pathways. This compound is valuable for research into cancer biology and therapeutic resistance. -
p-STAT3 Inhibitor
STAT3-IN-48 is a potent inhibitor of phosphorylated STAT3 (p-STAT3), functioning as a Sorafenib analogue. It effectively induces apoptosis in cancer cells through the inactivation of STAT3 via a SHP-1 dependent mechanism. Notably, STAT3-IN-48 does not inhibit general kinase activity, highlighting its specificity. This reagent is suitable for research applications focused on cancer biology and targeting STAT3 signaling pathways. -
STAT3/5 Inhibitor
UC-514321 is a potent inhibitor of STAT3 and STAT5, effectively repressing TET1 expression without affecting TET2 or TET3. This compound demonstrates significant promise for the treatment of acute myeloid leukemia (AML) in both in vitro and in vivo settings. Its selective action and low toxicity profile make it a valuable tool for research in cancer therapeutics. -
STAT3 inhibitor
C188 is a selective STAT3 inhibitor that disrupts STAT3 SH2/pY-peptide binding and inhibits IL-6-mediated STAT3 phosphorylation, with an IC50 of 20 µM. This compound effectively prevents the nuclear-to-cytoplasmic translocation of STAT3, thereby promoting apoptosis in breast cancer cell lines exhibiting constitutive STAT3 activation. C188 demonstrates potent biological activity with EC50 values of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively, highlighting its potential applications in cancer research. -
STAT3 Inhibitor
LY5 is a potent inhibitor of STAT3, exhibiting an IC50 of 0.5 μM. It induces apoptosis and effectively inhibits STAT3 phosphorylation, demonstrating significant antitumor activity in vivo. This compound is utilized in cancer research to explore the mechanisms of STAT3-related signaling pathways and their implications in tumorigenesis. -
STAT3 Inhibitor
HJC0123 is a potent STAT3 inhibitor that effectively suppresses the proliferation of hepatic stellate cells while inducing cell cycle arrest and apoptosis. It reduces STAT3 phosphorylation, nuclear translocation, and transcriptional activity, leading to increased IL-6 production and inhibition of Smad2/3 phosphorylation, along with down-regulation of SOCS3. HJC0123 serves as a valuable tool for investigating liver fibrosis and related pathways. -
STAT3 Inhibitor
STAT3-IN-38 is a selective inhibitor of the signal transducer and activator of transcription 3 (STAT3) protein, exhibiting a KD value of 45.33 µM. By binding to the SH2 domain of STAT3, it effectively inhibits phosphorylation at the pTyr705 site, leading to the downregulation of downstream genes such as Survivin and Mcl-1. This compound has demonstrated the ability to block cell-cycle progression and induce apoptosis in colorectal cancer cells, making it a valuable tool for cancer research and therapeutic development. -
AKR1B1/STAT3/SLC7A11-Regulator
AKR1B1/STAT3/SLC7A11-regulator-1 is a regulatory compound that targets the AKR1B1, STAT3, and SLC7A11 pathways to enhance ferroptosis activity. This mechanism effectively reverses doxorubicin resistance in MCF-7/ADR breast cancer cells. It serves as a valuable tool in breast cancer research, particularly for studies focused on overcoming chemotherapy resistance and exploring ferroptosis as a therapeutic strategy. -
IKK/STAT3 Dual Inhibitor
ACHP is a selective IκB kinase (IKK) and STAT3 dual inhibitor, demonstrating potent inhibitory activity with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. It effectively disrupts the STAT3 signaling pathway, leading to cancer cell cycle arrest and apoptosis. Additionally, ACHP exhibits significant anti-inflammatory properties in preclinical models, such as the mouse ear edema model. This compound is a valuable tool for research in anti-inflammatory and anti-cancer studies, including applications in multiple myeloma and leukemia. -
HDAC3/p-STAT3 Inhibitor
1-Stearoyl-sn-glycero-3-phosphocholine is an inhibitor of histone deacetylase 3 (HDAC3) and the phosphorylation of signal transducer and activator of transcription 3 (p-STAT3). This compound has demonstrated the ability to induce apoptosis and exhibits significant anticancer activity in chronic myelogenous leukemia (CML) K562 cells. It serves as a valuable tool for researchers investigating the therapeutic potential of HDAC inhibitors in cancer treatment. -
STAT3/JAK Inhibitor
Brevilin A is a potent inhibitor of the STAT3/JAK signaling pathway, with an IC50 value of approximately 10.6 μM for STAT3. It exhibits anti-tumor properties and effectively inhibits the proliferation of cancer cells. Additionally, Brevilin A has been shown to induce both apoptosis and autophagy, making it a valuable tool for cancer research and therapeutic investigations. -
Stat5a/b Inhibitor
IST5-002 is a selective inhibitor of Stat5a and Stat5b, with IC50 values of 1.5 μM and 3.5 μM, respectively. This compound effectively disrupts the transcriptional activity of Stat5 proteins, inducing apoptosis in prostate cancer and chronic myeloid leukemia (CML) cells. IST5-002 is suitable for research applications focused on understanding the role of Stat5 in cancer progression and therapeutic targeting in prostate cancer and CML. -
STAT3 Inhibitor
Danvatirsen is an antisense oligonucleotide that specifically inhibits STAT3, a transcription factor involved in cell survival and proliferation. This compound reduces cell viability and promotes apoptosis in leukemia cell lines, while downregulating the expression of endogenous STAT3 and its downstream target genes. Additionally, Danvatirsen effectively diminishes proliferation and tumorigenicity in models of neuroblastoma and lymphoma. In vivo studies demonstrate its capacity to inhibit tumor growth rates in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen is applicable in research focused on lymphoma, myelodysplastic syndrome, acute myeloid leukemia, and neuroblastoma. -
STAT3 Inhibitor
HP590 is a potent, orally active inhibitor of STAT3, demonstrating an IC50 of 27.8 nM for STAT3 luciferase activity and 24.7 nM for ATP inhibition. This compound exhibits significant anti-proliferative effects on gastric cancer cells and effectively induces apoptosis. HP590 serves as a valuable research tool for investigating the role of STAT3 in cancer biology and potential therapeutic interventions. -
STAT3 Signal Inhibitor
STAT3-IN-12 is a potent inhibitor of the STAT3 signaling pathway, effectively blocking IL-6 induced JAK/STAT3 activation. This compound exhibits significant anti-cancer activity by inhibiting cell growth, reducing migration, promoting apoptosis, and inducing cell cycle arrest. STAT3-IN-12 is particularly relevant for research applications in cancers such as hepatocellular carcinoma (HCC) and esophageal carcinoma. -
STAT3 Phosphorylation Inhibitor
Tetramethylcurcumin is a selective inhibitor of STAT3 phosphorylation, targeting Janus kinase 2 and the Src homology-2 domain of STAT3. This compound demonstrates significant anti-inflammatory and anti-cancer properties, making it a valuable tool for research into cancer biology and inflammatory pathways. Its ability to modulate key signaling events provides insight into therapeutic strategies for diseases driven by aberrant STAT3 activity. -
STAT3 Inhibitor
STAT3-IN-11 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3), specifically targeting the phosphorylation at Tyr705. This compound downregulates the phosphorylation of downstream genes such as Survivin and Mcl-1, while leaving upstream tyrosine kinases like Src and JAK2 unaffected. By inducing apoptosis in cancer cells, STAT3-IN-11 presents potential as a valuable tool for research in cancer therapeutics and the development of effective STAT3 inhibitors. -
AKR1C1/JAK2/STAT3/NF-κB Inhibitor
Zingiberen Newsaponin is a potent inhibitor of the AKR1C1/JAK2/STAT3 and NF-κB signaling pathways. This steroid saponin compound demonstrates significant anti-hepatocellular carcinoma (HCC) activity by promoting cancer cell apoptosis through the induction of oxidative stress, as evidenced by the upregulation of ROS and MDA levels. Additionally, Zingiberen Newsaponin mitigates cerebral ischemia-reperfusion injury by reducing pro-inflammatory cytokines and enhancing superoxide dismutase (SOD) activity, thereby protecting neuronal cells. Furthermore, it has been shown to induce platelet aggregation, broadening its application in cardiovascular research. -
STAT3-SH2 Domain Inhibitor
STAT3-SH2 Domain Inhibitor 1 specifically targets the Src Homology 2 (SH2) domain of STAT3, exhibiting a Kd value of 1.57 μM. This compound effectively inhibits STAT3 signaling and transcriptional activation, leading to apoptosis in gastric cancer cells. It serves as a valuable tool for researching mechanisms of cancer progression and potential therapeutic strategies targeting the STAT3 pathway. -
STAT3 Inhibitor
8-Epixanthatin is a STAT3 inhibitor derived from Xanthium chinese Mill. It effectively inhibits STAT3 activation, leading to the induction of apoptosis in cancer cells. This compound demonstrates notable anti-tumor activity, making it a valuable tool for research applications focused on cancer biology and therapeutic development. -
STAT3 Inhibitor
WB436B is a selective inhibitor of STAT3, targeting STAT3-Tyr705 phosphorylation and modulating the expression of downstream STAT3 target genes. This compound exhibits significant cytotoxicity against pancreatic cancer cells while promoting apoptosis. In preclinical mouse models, WB436B has been shown to suppress tumor growth and metastasis, leading to an extended survival rate in tumor-bearing subjects. This makes WB436B a valuable tool for research in cancer biology and therapeutic development. -
STAT3 Inhibitor
HJC0416 hydrochloride is a potent inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3) that exhibits enhanced anticancer properties compared to Stattic. This compound has demonstrated significant biological activity against breast cancer, making it a promising candidate for cancer research applications. Its oral bioavailability and efficacy highlight its potential as a valuable tool for investigating STAT3-related pathways in oncology. -
STAT3 Inhibitor
SC99 is a selective inhibitor of the STAT3 pathway, exerting its effects through the inhibition of JAK2. By binding to the ATP-binding pocket of JAK2, SC99 effectively prevents the phosphorylation of both JAK2 and STAT3, while sparing other kinases linked to STAT3 signaling. SC99 demonstrates significant biological activity, including the inhibition of platelet activation and aggregation, as well as potent anti-myeloma and anti-thrombotic effects, making it a valuable tool for research in cancer and cardiovascular studies. -
STAT3 Inhibitor
LLL3 is a potent STAT3 inhibitor that effectively impedes the dimerization and phosphorylation of STAT3, thereby blocking its translocation into the nucleus. This mechanism leads to reduced expression of STAT3-dependent genes, including those encoding Bcl-xL and cyclin D1. Moreover, LLL3 has been shown to induce growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells through the activation of the caspase pathway. This reagent is valuable for investigating cancers associated with persistent STAT3 activation. -
STAT5b Inhibitor
Pomstafib-2 is a potent and selective inhibitor of STAT5b, a transcription factor involved in various signaling pathways. This compound reduces the expression of phosphorylated STAT5b (pSTAT5b) and promotes apoptotic processes in cells. Pomstafib-2 is valuable for studying STAT5b-related biological functions and developing therapies targeting STAT5b-driven malignancies. -
STAT1 Enhancer
2-Nitrophenol (2-NP) is a selective enhancer of STAT1 transcription, acting primarily through modulation of interferon signaling pathways. This compound has been shown to augment the ability of IFN-γ to inhibit cell proliferation in human breast cancer and fibrosarcoma models. Its application in research focuses on elucidating the mechanisms of STAT1-related pathways and developing potential therapeutic strategies for cancer treatment. -
JAK2/STAT3/NF-κB Inhibitor
Reticuline acts as a JAK2/STAT3 and NF-κB signaling pathway inhibitor, displaying notable anti-inflammatory properties. It effectively downregulates the mRNA expression of pro-inflammatory cytokines such as TNF-α and IL-6 while also reducing the phosphorylation levels of JAK2 and STAT3. Additionally, Reticuline demonstrates potential cardiovascular effects, making it a valuable tool for research in inflammation and cardiovascular studies. -
α7 nAchR/JAK2/STAT3 Agonist
α7 nAchR-JAK2-STAT3 agonist 1 is a selective agonist targeting the α7 nicotinic acetylcholine receptor, modulating the JAK2-STAT3 signaling pathway. It demonstrates significant anti-inflammatory activity by inhibiting the expression of inducible nitric oxide synthase (iNOS), interleukin-1 beta (IL-1β), and interleukin-6 (IL-6) in murine RAW264.7 macrophages, with an IC50 of 0.32 μM for nitric oxide production. Additionally, it effectively suppresses lipopolysaccharide (LPS)-induced nitric oxide release, NF-κB activation, and related cytokine production. This compound is valuable for studying sepsis and inflammatory responses. -
JAK2/STAT3 Inhibitor
SD-1029 is a selective JAK2/STAT3 inhibitor that impedes the phosphorylation of JAK2, thereby obstructing STAT3 activation. By inhibiting STAT3 nuclear translocation, SD-1029 serves as a valuable tool for studying the JAK2/STAT3 signaling pathway. This compound is relevant in research applications involving cancer, autoimmune disorders, and other diseases associated with dysregulated STAT3 activity. -
JAK2/STAT3 Pathway Inhibitor
WP1193 is a potent inhibitor of the JAK2/STAT3 signaling pathway. It effectively suppresses the phosphorylation of both JAK2 and STAT3, leading to a decrease in the expression of key stem cell markers such as CD133 and c-myc. This compound is valuable for research into glioblastoma and other cancers associated with aberrant activation of the JAK2/STAT3 pathway. -
JAK/STAT Inhibitor
JAK-STAT-IN-1 is a selective inhibitor of the JAK-STAT signaling pathway. This compound exhibits potent inhibitory activity, making it a valuable tool in the investigation of autoimmune disorders. Its specificity for JAK-STAT modulation facilitates research into the underlying mechanisms of inflammation and immune response regulation. -
JAK2/STAT3 Iinhibitor
HD-2a is a JAK2/STAT3 inhibitor that functions by downregulating circDcbld2 expression in RAW264.7 cells. This compound is valuable for research into the modulation of the JAK2/STAT3 signaling pathway, which is implicated in various inflammatory and autoimmune disorders. HD-2a can aid in the exploration of therapeutic strategies targeting JAK2/STAT3-mediated processes. -
JAK2-STAT5 Activator
Methionyl-methionine (Met-Met) functions as a JAK2-STAT5 activator, enhancing intracellular substrate availability. This compound has been shown to significantly promote the expression of α-s1 casein (αS1-CN) in mammary explants, mediated through the activation of JAK2-STAT5 and mTOR signaling pathways. Its role in modulating these critical pathways makes it a valuable tool for research in lactation biology and protein synthesis studies. -
IRS1/2/STAT3 Inhibitor
NT219 is a potent dual inhibitor of insulin receptor substrates 1 and 2 (IRS1/2) and signal transducer and activator of transcription 3 (STAT3). It disrupts IRS1/2 degradation and inhibits STAT3 phosphorylation, impacting essential signaling pathways associated with various oncogenic processes. NT219 is relevant for research applications focused on cancer biology, particularly in understanding the interplay of these critical signaling molecules in tumor progression and resistance. -
STAT3 Inhibitor
STAT3-IN-9 is a selective inhibitor of STAT3, specifically targeting its activation by preventing Tyr705 phosphorylation while leaving STAT1 (Tyr701) unphosphorylated. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. It can be effectively utilized in research applications focusing on cancer biology and the role of STAT3 in tumor progression. -
STAT3 Inhibitor
STAT3-IN-53 is a selective inhibitor of STAT3, targeting its SH2 domain with a Kd value of 6.16 μM. This compound effectively suppresses phosphorylation at the Y705 site, thereby inhibiting the IL-6/JAK/STAT3 signaling pathway. By downregulating the transcription and expression of critical oncogenes such as cyclin D1 and c-Myc, STAT3-IN-53 induces cell cycle arrest and promotes apoptosis, demonstrating potential anticancer activity, particularly in colorectal cancer research applications. -
STAT3 Inhibitor
STAT3-IN-18 is a STAT3 inhibitor that selectively targets the JAK2-STAT3 signaling pathway, demonstrating significant anti-proliferative effects in breast cancer cells. This compound promotes apoptotic cell death through the activation of caspase-3 and increases cleaved polyADP-ribose polymerase levels. Additionally, STAT3-IN-18 enhances the maturation and antigen presentation of dendritic cells, while exhibiting favorable safety profiles in vivo, making it a valuable tool for cancer research and immunotherapy studies. -
Miticide/STAT3 Inhibitor
Fluacrypyrim is a potent miticide that functions as a selective inhibitor of the STAT3 signaling pathway. It effectively induces growth arrest and apoptosis in STAT3-dependent cancer cells by significantly decreasing cyclin D1 protein and mRNA levels, leading to G1 cell cycle arrest. Additionally, Fluacrypyrim mitigates irradiation-induced hematopoietic system injury by protecting hematopoietic stem cells from apoptosis. Its analgesic and anti-inflammatory properties are demonstrated through the inhibition of uterine smooth muscle contraction and inflammatory responses, making it a valuable reagent for cancer and inflammation research. -
STAT3 Inhibitor
STAT3-IN-10 is a selective inhibitor of the Signal Transducer and Activator of Transcription 3 (STAT3), exhibiting an IC50 value of 5.18 µM. This compound directly interacts with the SH2 domain of STAT3, leading to the induction of apoptosis in cancer cells. STAT3-IN-10 is ideal for research applications focused on elucidating STAT3 signaling pathways and exploring therapeutic strategies for cancer treatment.

