1. Search Result

Search Result

Pathways Recommended: JAK/STAT Signaling
Targets Recommended: STAT JAK

Results for "Alopecia jak stat Inhibitors" in MCE Product Catalog:

223

Inhibitors & Agonists

4

Screening Libraries

1

Dye Reagents

7

Peptides

46

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-131140
    BD750

    JAK STAT Cancer Inflammation/Immunology
    BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
  • HY-116505
    JAK1-IN-4

    JAK Cancer
    JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM).
  • HY-125970
    CRTh2 antagonist 2

    Prostaglandin Receptor Endocrinology
    CRTh2 antagonist 2 is selective and potent CRTH2 antagonist extracted from patent US20140148470A1, compound Example 1, has an IC50 of ≤10 nM. CRTh2 antagonist 2 can be used in research of androgenic alopecia.
  • HY-101853
    STAT5-IN-1

    STAT Cancer
    STAT5-IN-1 is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.
  • HY-136658
    STAT3-IN-7

    STAT Apoptosis Cancer
    STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects.
  • HY-128588
    STAT3-IN-3

    STAT Cancer
    STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3).
  • HY-100753
    STAT3-IN-1

    STAT Apoptosis Cancer
    STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor apoptosis.
  • HY-102048
    STAT5-IN-2

    STAT Cancer
    STAT5-IN-2 is a STAT5 inhibitor with EC50s of 9 μM and 5 μM in K562 and KU812 cells, respectively. Potent antileukemic effect.
  • HY-13827
    JAK-IN-1

    JAK Inflammation/Immunology
    JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
  • HY-111750
    JAK-IN-3

    JAK Inflammation/Immunology
    JAK-IN-3 (compound 22) is a potent JAK inhibitor, with IC50 values of 3 nM, 5 nM, 34 nM and 70 nM for JAK3, JAK1, TYK2 and JAK2, respectively.
  • HY-100759
    JAK2-IN-4

    JAK Cancer
    JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively.
  • HY-19544
    JAK3-IN-1

    JAK Cancer
    JAK3-IN-1 is a potent, selective and orally active JAK3 inhibitor with an IC50 of 4.8 nM. JAK3-IN-1 shows over 180-fold more selective for JAK3 than JAK1 (IC50 of 896 nM) and JAK2 (IC50 of 1050 nM).
  • HY-111471
    JAK-IN-5

    JAK Inflammation/Immunology
    JAK-IN-5 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
  • HY-111749
    JAK-IN-4

    JAK Inflammation/Immunology
    JAK-IN-4 is a prodrug of a JAK inhibitor, effective in murine collagen induced arthritis model.
  • HY-101976
    JAK3-IN-6

    JAK Inflammation/Immunology
    JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
  • HY-126141
    JAK/HDAC-IN-1

    JAK HDAC Cancer
    JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.
  • HY-12000
    AG-490

    Tyrphostin AG 490

    EGFR STAT Autophagy Cancer
    AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
  • HY-U00390
    JAK3-IN-7

    JAK Cancer
    JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
  • HY-126294
    JAK1-IN-7

    JAK Inflammation/Immunology
    JAK1-IN-7 is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.
  • HY-113573
    Protosappanin A

    PTA

    JAK STAT Inflammation/Immunology
    Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.
  • HY-119935
    JAK3 covalent inhibitor-1

    JAK Inflammation/Immunology
    JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
  • HY-111471A
    JAK-IN-5 hydrochloride

    JAK Inflammation/Immunology
    JAK-IN-5 hydrochloride is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
  • HY-U00318
    JAK-IN-11

    JAK Inflammation/Immunology
    JAK-IN-11 is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment.
  • HY-N1405
    Cucurbitacin I

    Elatericin B; JSI-124; NSC-521777

    STAT JAK Cancer
    Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
  • HY-130247
    JAK2/FLT3-IN-1

    JAK FLT3 Cancer
    JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.
  • HY-15312
    WP1066

    STAT JAK Apoptosis Cancer
    WP1066 is an inhibitor of JAK2 and STAT3, and also shows effect on STAT5 and ERK1/2, without affecting JAK1 and JAK3.
  • HY-N1356
    Reticuline

    JAK STAT NF-κB Inflammation/Immunology
    Reticuline, isolated from Litsea cubeba, shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3.
  • HY-U00277
    JAK-IN-10

    JAK Others
    JAK-IN-10 is a useful composition for treating and/or preventing dry eye disorders.
  • HY-15480
    NSC 42834

    jak2 Inhibitor V; Z3

    JAK Cancer
    NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.
  • HY-N2527
    Sanshool

    Autophagy Inflammation/Immunology
    Sanshool is a major component in Zanthoxylum bungeanum. Sanshool improves UVB-induced skin photodamage by targeting JAK2/STAT3-dependent autophagy.
  • HY-N0635
    Prim-O-glucosylcimifugin

    NO Synthase COX Inflammation/Immunology
    Prim-O-glucosylcimifugin exerts anti-inflammatory effects through the inhibition of iNOS and COX-2 expression by through regulating JAK2/STAT3 signaling.
  • HY-100544
    FLLL32

    STAT JAK Apoptosis Cancer
    FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
  • HY-15508
    JANEX-1

    WHI-P131; jak3 inhibitor I

    JAK Cancer
    JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
  • HY-14722C
    NVP-BSK805 trihydrochloride

    JAK Cancer
    NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  • HY-14722A
    NVP-BSK805 dihydrochloride

    JAK Cancer
    NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  • HY-14722
    NVP-BSK805

    JAK Cancer
    NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
  • HY-112724
    SHR0302

    JAK Apoptosis Cancer Inflammation/Immunology
    SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
  • HY-107429
    Abrocitinib

    PF-04965842

    JAK Inflammation/Immunology
    Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease.
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent,orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-N1535
    Ponicidin

    Rubescensine B

    Apoptosis Cancer Inflammation/Immunology
    Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3.
  • HY-N1447
    Ganoderic acid A

    Apoptosis Autophagy Endogenous Metabolite Cancer
    Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.
  • HY-136336
    Tofacitinib metabolite-1

    Drug Metabolite Others
    Tofacitinib metabolite-1 is a metabolite of Tofacitinib (HY-40354), a JAK inhibitor. Tofacitinib metabolite-1 can be used in the pharmacokinetics and metabolism studies of tofacitinib.
  • HY-15999A
    Cerdulatinib hydrochloride

    PRT062070 hydrochloride; PRT2070 hydrochloride

    Syk JAK Cancer
    Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-N2907
    Atranorin

    Ras Endogenous Metabolite Cancer
    Atranorin is a lichen secondary metabolite. Atranorin inhibits lung cancer cell motility and tumorigenesis by affecting AP-1, Wnt, and STAT signaling and suppressing RhoGTPase activity.
  • HY-N0678
    Icaritin

    Anhydroicaritin

    Autophagy Apoptosis Cancer
    Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis[3.
  • HY-N2959
    Brevilin A

    JAK STAT Apoptosis Autophagy Cancer
    Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
  • HY-U00376
    5α-reductase-IN-1

    Others Metabolic Disease
    5α-reductase-IN-1 is an inhibitor of 5α-reductase, used for the research of patterned alopecia in combination with minoxidil.
  • HY-B0141A
    Alpha-Estradiol

    Alfatradiol; Epiestradiol; Epiestrol

    5 alpha Reductase Endogenous Metabolite Inflammation/Immunology
    Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
  • HY-N0705
    Curculigoside

    JAK STAT NF-κB Inflammation/Immunology Neurological Disease Cancer
    Curculigoside is the main saponin in C. orchioide, exerts significant antioxidant, anti-osteoporosis, antidepressant and neuroprotection effects. Curculigoside possesses significant anti-arthritic effects in vivo and in vitro via regulation of the JAK/STAT/NF-κB signaling pathway.
  • HY-N0781
    Linderalactone

    Apoptosis Cancer
    Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
  • HY-102084
    LMT-28

    Interleukin Related Inflammation/Immunology
    LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
  • HY-W063968
    RO8191

    RO4948191

    IFNAR JAK STAT HCV Infection
    RO8191 (RO4948191), an imidazonaphthyridine compound, is an orally active and potent interferon (IFN) receptor agonist. RO8191 activates IFN-stimulated genes (ISGs) expression and JAK/STAT phosphorylation. RO8191 shows antiviral activity against both HCV and EMCV with an IC50 of 200 nM for HCV replicon.
  • HY-N0201
    Atractylenolide I

    Toll-like Receptor (TLR) JAK STAT Cancer
    Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
  • HY-13961
    GLPG0634 analog

    JAK Cancer
    GLPG0634 (analog) (compound176)is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.
  • HY-N2515
    Ginsenoside Rk1

    NF-κB PI3K JAK Apoptosis Cancer Inflammation/Immunology
    Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures. Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB. Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis. Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
  • HY-10963
    Momelotinib Mesylate

    CYT387 (Mesylate)

    JAK Autophagy Cancer
    Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
  • HY-16975
    SH-4-54

    STAT Cancer
    SH-4-54 is a STAT inhibitor that binds to STAT3 and STAT5 with KDs of 300, 464 nM, respectively.
  • HY-10961
    Momelotinib

    CYT387

    JAK Autophagy Apoptosis Cancer
    Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
  • HY-18300
    Filgotinib

    GLPG0634

    JAK Cancer
    Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
  • HY-15315A
    Baricitinib phosphate

    LY3009104 phosphate; INCB028050 phosphate

    JAK Inflammation/Immunology
    Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
  • HY-12469
    Decernotinib

    VX-509; VRT-831509

    JAK Inflammation/Immunology
    Decernotinib is a potent, orally active JAK3 inhibitor, with Kis of 2.5, 11, 13 and 11 nM for JAK3, JAK1, JAK2, and TYK2, respectively.
  • HY-10962
    Momelotinib sulfate

    CYT387 sulfate salt

    JAK Autophagy Apoptosis Cancer
    Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
  • HY-116035
    Nimbolide

    NF-κB CDK Apoptosis Cancer
    Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.
  • HY-14435
    Pyridone 6

    JAK Cancer
    Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
  • HY-19568
    Peficitinib

    ASP015K; JNJ-54781532

    JAK Inflammation/Immunology Cancer
    Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-N0193
    Artesunate

    STAT Ferroptosis Parasite Virus Protease Cancer
    Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
  • HY-50856
    Ruxolitinib

    INCB18424

    JAK Autophagy Mitophagy Apoptosis Cancer
    Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.
  • HY-50859
    Ruxolitinib sulfate

    INCB018424 sulfate

    JAK Autophagy Cancer
    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
  • HY-109053
    Delgocitinib

    JTE-052

    JAK Inflammation/Immunology
    Delgocitinib (JTE-052) is a specific JAK inhibitor with IC50s of 2.8, 2.6, 13 and 58 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
  • HY-16997
    Itacitinib

    INCB039110

    JAK Cancer
    Itacitinib (INCB039110) is an orally active and selective inhibitor of JAK1 with an IC50 of 2 nM for human JAK1. Itacitinib shows >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
  • HY-100895
    SAR-20347

    JAK Cancer
    SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC50s of 0.6, 23, 26 and 41 nM, respectively.
  • HY-11067
    WHI-P97

    JAK Inflammation/Immunology
    WHI-P97 is a rationally designed potent inhibitor of JAK-3.
  • HY-101024
    PF-06263276

    JAK Inflammation/Immunology
    PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively.
  • HY-13818
    Stattic

    STAT Apoptosis Cancer Inflammation/Immunology
    Stattic is a potent STAT3 inhibitor. Stattic inhibits STAT3 phosphorylation (at Y705 and S727).
  • HY-P2282
    APTSTAT3-9R

    STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity.
  • HY-13450
    ZM 449829

    JAK Inflammation/Immunology
    ZM 449829 is a potent, selective and ATP competitive inhibitor of JAK3, with a pIC50 of 6.8. ZM 449829 will be useful pharmacological tools for the investigation of the JAK3.
  • HY-19631B
    Ilginatinib hydrochloride

    NS-018 hydrochloride

    JAK Cancer
    Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-19631A
    Ilginatinib

    NS-018

    JAK Cancer
    Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-19631
    Ilginatinib maleate

    NS-018 maleate

    JAK Cancer
    Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
  • HY-102046
    FM-381

    JAK Inflammation/Immunology
    FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-15270
    BMS-911543

    JAK Cancer
    BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).
  • HY-18061
    Ochromycinone

    (Rac)-STA-21

    STAT Bacterial Cancer Infection
    Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.
  • HY-10410
    TG101209

    FLT3 JAK RET Autophagy Apoptosis Cancer
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
  • HY-10409
    Fedratinib

    TG-101348; SAR 302503

    JAK Apoptosis Cancer
    Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
  • HY-10409A
    Fedratinib hydrochloride hydrate

    TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate

    JAK Apoptosis Cancer
    Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.
  • HY-B0667
    Balsalazide

    Interleukin Related STAT Cancer Inflammation/Immunology
    Balsalazide could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
  • HY-B0667A
    Balsalazide sodium hydrate

    Balsalazide disodium dihydrate

    Interleukin Related STAT Inflammation/Immunology Cancer
    Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
  • HY-40354
    Tofacitinib

    Tasocitinib; CP-690550

    JAK Apoptosis Inflammation/Immunology Cancer
    Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.
  • HY-107361
    AZD4205

    JAK Cancer
    AZD4205 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM).
  • HY-50858
    Ruxolitinib phosphate

    INCB018424 phosphate

    JAK Autophagy Mitophagy Cancer
    Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
  • HY-120469
    GDC-046

    JAK Inflammation/Immunology
    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
  • HY-131014
    FM-479

    JAK Inflammation/Immunology
    FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases. FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
  • HY-136546
    Stafia-1

    STAT Cancer
    Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-13577A
    Oclacitinib maleate

    PF-03394197 maleate

    JAK Inflammation/Immunology
    Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
  • HY-16755
    Solcitinib

    GSK-2586184; GLPG-0778

    JAK Inflammation/Immunology
    Solcitinib is an orally active, competitive, potent, selective JAK1 inhibitor, with an IC50 of 9.8 nM, and 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively; Solcitinib is used in the research of moderate-to-severe plaque-type psoriasis.
  • HY-18960
    CHZ868

    JAK Cancer
    CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
  • HY-112708
    PF-06700841

    JAK Inflammation/Immunology
    PF-06700841 is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
  • HY-15315
    Baricitinib

    LY3009104; INCB028050

    JAK Inflammation/Immunology
    Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
  • HY-129602
    SD-36

    PROTAC STAT Apoptosis Cancer
    SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-10193
    AZD-1480

    JAK Cancer
    AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively.
  • HY-126290A
    Tyk2-IN-9

    JAK Inflammation/Immunology
    Tyk2-IN-9 is a potent,selective and specific inhibitor of JAK kinases, inhibits Tyk2, JAK1 and JAK2 with IC50 values of 6 nM, 21nM and 6nM, respectively. Tyk2-IN-9, example 19, is extracted from patent US2017240552A1.
  • HY-112708A
    PF-06700841 P-Tosylate

    JAK Inflammation/Immunology
    PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
  • HY-15166
    SB1317

    TG02

    CDK JAK FLT3 Cancer
    SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
  • HY-18009
    LFM-A13

    Btk Polo-like Kinase (PLK) JAK Cancer
    LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
  • HY-100614
    AS1517499

    STAT Inflammation/Immunology Cancer
    AS1517499 is a potent STAT6 inhibitor with an IC50 of 21 nM.
  • HY-40354A
    Tofacitinib citrate

    Tasocitinib citrate; CP-690550 citrate

    JAK Apoptosis Bacterial Fungal Influenza Virus Cancer Infection Inflammation/Immunology
    Tofacitinib citrate is an orally available JAK1/2/3 inhibitor with IC50s of 1, 20, and 112 nM, respectively. Tofacitinib citrate has antibacterial, antifungal and antiviral activities.
  • HY-108264
    TCS 21311

    NIBR3049

    JAK PKC GSK-3 Cancer
    TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
  • HY-129603
    SI-109

    STAT Ligand for Target Protein for PROTAC Cancer
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
  • HY-15146
    NSC 74859

    S3I-201

    STAT Cancer
    NSC 74859 is a selective Stat3 inhibitor with an IC50 of 86 μM.
  • HY-112288
    C188-9

    STAT Cancer
    C188-9 is a Stat3 inhibitor, with a Kd of 4.7 nM.
  • HY-12987S
    Pimozide D4

    R6238 D4

    Dopamine Receptor Adrenergic Receptor STAT Cancer Endocrinology Neurological Disease
    Pimozide D4 (R6238 D4) is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-10411
    AZ960

    JAK Apoptosis Parasite Virus Protease Cancer
    AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
  • HY-100602
    HJC0152 hydrochloride

    STAT Apoptosis Cancer
    HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
  • HY-P1061
    Colivelin

    STAT Amyloid-β Neurological Disease
    Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
  • HY-112442
    AZ-3

    JAK Cancer
    AZ-3 is a potent and selective JAK1 inhibitor with an IC50 of 34 nM.
  • HY-13919
    Napabucasin

    STAT Cancer
    Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
  • HY-15999
    Cerdulatinib

    PRT062070; PRT2070

    JAK Syk Cancer
    Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
  • HY-N2521
    Tetramethylcurcumin

    FLLL31

    STAT Apoptosis Cancer Inflammation/Immunology
    Tetramethylcurcumin (FLLL31), derived from curcumin, specifically suppresses the phosphorylation of STAT3 by binding selectively to Janus kinase 2 and the STAT3 Src homology-2 domain. Tetramethylcurcumin exhibits anti-inflammatory and anti-cancer effects.
  • HY-P1061A
    Colivelin TFA

    STAT Amyloid-β Neurological Disease
    Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
  • HY-19569
    Upadacitinib

    ABT-494

    JAK Inflammation/Immunology
    Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) is used in development for the treatment of several autoimmune disorders.
  • HY-12987
    Pimozide

    R6238

    Dopamine Receptor Adrenergic Receptor STAT Cancer Neurological Disease Endocrinology
    Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
  • HY-113066
    Guanosine 5'-diphosphate

    Endogenous Metabolite Inflammation/Immunology
    Guanosine 5'-diphosphate is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  • HY-100453
    HO-3867

    STAT Apoptosis Cancer
    HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.
  • HY-50856A
    Ruxolitinib (S enantiomer)

    S-Ruxolitinib; S-INCB18424

    JAK Cancer
    Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib S enantiomer is a JAK inhibitor
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt

    Endogenous Metabolite Inflammation/Immunology
    Guanosine 5'-diphosphate disodium salt is a nucleoside diphosphate. Guanosine 5'-diphosphate is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6)/stat-3 pathway.
  • HY-P1453
    CMD178

    STAT Cancer
    CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 also is an inhibitor of STAT5 and inhibit Treg cell development.
  • HY-P1453A
    CMD178 TFA

    STAT Inflammation/Immunology
    CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
  • HY-108419
    WHI-P258

    JNK Cancer
    WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM.
  • HY-103128
    inS3-54A18

    STAT Cancer
    inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.
  • HY-B1436
    Nifuroxazide

    STAT Bacterial Cancer Infection
    Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity.
  • HY-125355
    SEC

    Apoptosis Cancer
    SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-18293
    NSC 33994

    JAK Cancer
    NSC 33994 (G6) is a selective JAK2 inhibitor, with an IC50 of 60 nM.
  • HY-126242S
    Tyk2-IN-7

    JAK Inflammation/Immunology
    Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki.app of 0.00053 μM and 0.00007 μM, respectively. Tyk2-IN-7 (Compound 48) provides a highly selective alternative to conventional TYK2 orthosteric inhibitors, inhibits TYK2/JAK1/JAK2 kinase domain. Tyk2-IN-7 (Compound 48) provides robust inhibition in a mouse IL-12-induced IFNγ pharmacodynamic model as well as efficacy in an IL-23 and IL-12-dependent mouse colitis model.
  • HY-N0897
    Corylifol A

    Corylifol-A; Corylinin

    STAT Others
    Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
  • HY-120395
    UC-514321

    STAT Apoptosis Cancer Inflammation/Immunology
    UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.
  • HY-N0516
    Casticin

    Vitexicarpin

    STAT Inflammation/Immunology
    Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
  • HY-100493
    BP-1-102

    STAT Cancer
    BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC50 of 6.8 μM.
  • HY-N0038
    Alantolactone

    (+)-Alantolactone; Alant camphor; Inula camphor

    STAT Apoptosis TGF-beta/Smad Cancer
    Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.
  • HY-B0497B
    Niclosamide monohydrate

    BAY2353 monohydrate

    STAT Bacterial Antibiotic Infection
    Niclosamide monohydrate is an inhibitor of STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
  • HY-15343
    CEP-33779

    JAK Cancer
    CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
  • HY-100754
    PF-06651600

    JAK Inflammation/Immunology
    PF-06651600 is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM.
  • HY-50514
    AT9283

    JAK Aurora Kinase Bcr-Abl FLT3 Apoptosis Autophagy Cancer
    AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-16379
    Pacritinib

    SB1518

    FLT3 JAK Cancer
    Pacritinib is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
  • HY-100494
    SH5-07

    STAT Cancer
    SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay.
  • HY-N2240
    Eupalinolide K

    STAT Cancer
    Eupalinolide K, a sesquiterpene lactones compound from Eupatorium lindleyanum, is a STAT3 inhibitor. Eupalinolide K is a Michael reaction acceptor (MRA) .
  • HY-40354B
    (3S,4R)-Tofacitinib

    JAK Inflammation/Immunology
    (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
  • HY-40354D
    (3R,4S)-Tofacitinib

    JAK Inflammation/Immunology
    (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-N0174
    Cryptotanshinone

    Cryptotanshinon; Tanshinone c

    STAT Autophagy Cancer
    Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
  • HY-16997A
    Itacitinib adipate

    JAK Cancer
    Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
  • HY-40354C
    (3S,4S)-Tofacitinib

    JAK Inflammation/Immunology
    (3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
  • HY-N7452
    Coumermycin A1

    Bacterial Metabolic Disease
    Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
  • HY-N2312
    Mogrol

    ERK STAT Cancer
    Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.
  • HY-N6940
    Prosapogenin A

    Progenin III

    Apoptosis Cancer
    Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
  • HY-B0069
    Fludarabine

    F-ara-A; NSC 118218

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT Apoptosis Cancer
    Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which also inhibits phosphorylation of STAT1. Fludarabine, a pro-drug, is converted metabolically by dephosphorylation to the antimetabolite, F-ara-A.
  • HY-16196
    ENMD-119

    ENMD 1198; IRC 110160

    HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-119 is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity, and is suitable for inhibiting HIF-1α and STAT3 in human HCC cells.
  • HY-12589
    ZM39923 hydrochloride

    JAK Cancer Neurological Disease
    ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
  • HY-12589A
    ZM39923

    JAK Cancer Neurological Disease
    ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
  • HY-13895
    WHI-P154

    EGFR JAK Apoptosis Cancer
    WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC50s of 4 nM and 1.8 μM, respectively.
  • HY-N0177
    Diosgenin

    STAT Metabolic Disease
    Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57.
  • HY-10074
    TPCA-1

    IKK STAT Apoptosis Inflammation/Immunology Cancer
    TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-N0622
    Morusin

    Mulberrochromene

    NF-κB STAT Bacterial Cancer Infection Inflammation/Immunology
    Morusin is a prenylated flavonoid isolated from M. australis with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.
  • HY-N0751
    Scutellarin

    STAT Akt HIV Cancer Infection
    Scutellarin, an active flavone isolated from Scutellaria baicalensis, can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts. Scutellarin is active against HIV-1IIIB, HIV-1(74V) and HIV-1KM018 with EC50s of 26 μM, 253 μM and 136 μM, respectively.
  • HY-121418
    Lusianthridin

    c-Myc Cancer
    Lusianthridin, a pure compound from Dendrobium venustum, have an anti-migratory effect. Lusianthridin enhances c-Myc degradation through the inhibition of Src-STAT3 signaling.
  • HY-N6651
    Isocryptotanshinone

    STAT Phosphatase Cancer
    Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
  • HY-N4127
    3'-Demethylnobiletin

    Others Cancer
    3'-Demethylnobiletin, a derivative of Nobiletin, is a polymethoxyflavonoid in citrus fruits. Nobiletin exhibits anticancer activity and inhibits tumor angiogenesis by regulating Src, FAK, and STAT3 signaling.
  • HY-122214
    AC-73

    Autophagy Cancer
    AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-N1410
    Triacetylresveratrol

    STAT NF-κB Cancer
    Triacetylresveratrol, an acetylated analog of Resveratrol. Triacetylresveratrol decreases the phosphorylation of STAT3 and NF-κB in a dose- and time- dependent manner in PANC-1 and BxPC-3 cells. Anticancer effects.
  • HY-N0250
    Saikosaponin D

    STAT NF-κB Estrogen Receptor/ERR Bacterial Cancer Infection Inflammation/Immunology
    Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.
  • HY-12352A
    HJC0416 hydrochloride

    STAT Apoptosis Cancer
    HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study.
  • HY-125170
    Galiellalactone

    STAT Cancer
    Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer.
  • HY-101021
    Ascochlorin

    Ilicicolin D

    STAT Apoptosis Cancer Inflammation/Immunology
    Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
  • HY-13034
    Gandotinib

    LY2784544

    JAK FLT3 FGFR VEGFR Cancer
    Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
  • HY-B0497
    Niclosamide

    BAY2353

    STAT Parasite Antibiotic Infection Cancer
    Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
  • HY-B0497C
    Niclosamide olamine

    BAY2353 olamine

    STAT Parasite Antibiotic Autophagy
    Niclosamide olamine is an anthelmintic that disrupts mitochondrial metabolism in parasitic worms and animal models. Niclosamide olamine inhibits STAT3 (IC50 = 0.25 μM) and stimulates autophagy by reversibly inhibiting mammalian target of Rapamycin complex 1 (mTORC1) signaling.
  • HY-114495
    Caerulomycin A

    Cerulomycin; Caerulomycin

    Fungal Antibiotic Infection Inflammation/Immunology
    Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-13264
    Degrasyn

    WP1130

    Deubiquitinase Bcr-Abl Autophagy Apoptosis Cancer
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
  • HY-103018
    Gusacitinib

    ASN-002

    JAK Syk Cancer
    Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
  • HY-118532
    Tyrphostin AG30

    AG30

    EGFR Cancer
    Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
  • HY-50867
    Lestaurtinib

    CEP-701; KT-5555

    JAK FLT3 Trk Receptor Cancer
    Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
  • HY-N2116
    Ginkgolic acid C17:1

    PTEN Phosphatase Cancer
    Ginkgolic acid C17:1, extracted from Ginkgo biloba Leaves, suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid C17:1 has anticancer effects.
  • HY-136657
    SC-43

    STAT Phosphatase Apoptosis Cancer
    SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-111388A
    SEL120-34A monohydrochloride

    CDK Cancer
    SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
  • HY-43722
    Lenalidomide-Br

    Ligand for E3 Ligase Cancer
    Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
  • HY-101019
    Ossirene

    AS101

    Interleukin Related Caspase Cancer Inflammation/Immunology
    Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
  • HY-19759
    SRT 2183

    Sirtuin Apoptosis Cancer
    SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-N1280
    Semilicoisoflavone B

    Amyloid-β Neurological Disease
    Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β () secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.
  • HY-109854A
    (R)-Lisofylline

    (R)-Lisophylline

    STAT Metabolic Disease Inflammation/Immunology
    (R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
  • HY-N6843
    Arnicolide D

    Caspase PI3K Akt mTOR STAT Cancer
    Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
  • HY-N1987
    Cucurbitacin IIb

    Apoptosis Inflammation/Immunology
    Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • HY-13072
    Cenisertib

    AS-703569; R-763

    Aurora Kinase Bcr-Abl Akt STAT FLT3 Cancer
    Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.
  • HY-N6953
    Garcinone D

    STAT Keap1-Nrf2 Reactive Oxygen Species Neurological Disease
    Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners.
  • HY-120214
    TAS05567

    Syk Inflammation/Immunology
    TAS05567 is a potent, highly selective, ATP-competitive and orally active Syk inhibitor with an IC50 of 0.37 nM. In a panel of 192 kinases, TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR and RET with IC50s of 10 nM, 4.8 nM, 600 nM and 29 nM, respectively). TAS05567 can be used for humoral immune-mediated inflammatory conditions such as autoimmune and allergic diseases.
  • HY-16561
    Resveratrol

    trans-Resveratrol; SRT501

    IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Cancer Infection Inflammation/Immunology
    Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor.
  • HY-100671
    L002

    Histone Acetyltransferase STAT Cancer Inflammation/Immunology
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-N0498
    Nitidine chloride

    Parasite Apoptosis STAT Topoisomerase ERK FAK p38 MAPK NF-κB Cancer Inflammation/Immunology
    Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-126675A
    AS2863619

    CDK STAT Inflammation/Immunology
    AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-123823
    Nitroaspirin

    NCX 4016

    COX Apoptosis Cancer
    Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
  • HY-126675
    AS2863619 free base

    CDK STAT Inflammation/Immunology
    AS2863619 free base enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 free base is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-111553
    TAS0728

    EGFR Cancer
    TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, binds to HER2 at C805, inhibits its kinase activity, with an IC50 of 13 nM. TAS0728 shows IC50s of 4.9, 8.5, 31, 65, 33, 25, 86 and 36 nM for BMX, HER4, BLK, EGFR, JAK3, SLK, LOK and human HER2, respectively. TAS0728 also inhibits the phosphorylation of HER2, HER3, and downstream effectors, shows no obvious effect on EGFR. Antitumor activity.
  • HY-15504A
    RGB-286638 free base

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-15504
    RGB-286638

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-N6954
    Garcinone C

    ATM/ATR STAT CDK Cancer
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia Champ that is used as an anti-inflammatory, analgesia, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner.
  • HY-N2609
    7,4'-Dihydroxyflavone

    CCR NF-κB Inflammation/Immunology Endocrinology
    7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid isolated from Glycyrrhiza uralensis, the eotaxin/CCL11 inhibitor, has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2. 7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.