JAK/STAT Signaling
Targets for JAK/STAT Signaling
Products for JAK/STAT Signaling
- Cat.No. Product Name Information
- GC65572 EGFR Protein Tyrosine Kinase Substrate EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.
- GC64497 EGFR-IN-17 EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance.
- GC33195 EGFR-IN-2 EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
- GC19132 EGFR-IN-3 EGFR-IN-3 is a third-generation EGFR TKI, with GI50 values of 5 nM (EGFR L858R/T790M), 10 nM (EGFR del19) and 689 nM (EGFR WT), respectively. EGFR-IN-3 has the potential for NSCLC research.
- GC66428 EGFR-IN-5 EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively.
- GC68440 EGFR-IN-69
- GC35966 EGFR-IN-7 EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 shows anti-tumor activity. EGFR-IN-7 can be used for the research of various cancers.
- GC65974 EGFR-IN-9 EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity.
- GC33170 ENMD-119 (ENMD 1198) ENMD-119 (ENMD 1198) (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-119 (ENMD 1198) is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
- GC33048 Epertinib (S-22611) Epertinib (S-22611) (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib (S-22611) shows potent antitumor activity.
- GC38350 Epertinib hydrochloride Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
- GC36003 Erlotinib mesylate EGFR inhibitor
- GC36016 Eupalinolide K Eupalinolide K, a sesquiterpene lactones compound from Eupatorium lindleyanum, is a STAT3 inhibitor. Eupalinolide K is a Michael reaction acceptor (MRA) .
- GC65992 FGFR2-IN-3 FGFR2-IN-3 is an orally active selective inhibitor of FGFR2.
- GC65991 FGFR2-IN-3 hydrochloride FGFR2-IN-3 hydrochloride is an orally active selective inhibitor of FGFR2.
- GC36044 FIIN-3 FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
- GC16875 FLLL32 STAT3 inhibitor
- GC14144 Fludarabine DNA synthsis inhibitor
- GC15134 Fludarabine Phosphate (Fludara) Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
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GC19408
FM381
FM-381 is a highly potent and JAK3-selective janus kinase (JAK) inhibitor
- GC38044 Fraxinellone
- GC13285 Galiellalactone inhibits IL-6-mediated JAK/STAT signal transduction
- GN10696 Garcinone C
- GN10741 Garcinone D
- GC32958 GDC-0339 GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
- GC68378 GDC-4379
- GC19509 Gefitinib-based PROTAC 3 A VHL-recruiting PROTAC
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GC14102
Genistein
Genistein is an isoflavone belonging to the flavonoid group of compounds and is found in a number of plants.
- GC12579 GLPG0634 GLPG0634 (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
- GC17222 GLPG0634 analogue GLPG0634 analogue (Compoun 176) is a broad spectrum JAK inhibitor with IC50 values of <100 nM against JAK1, JAK2 and JAK3.
- GC33253 GNE-955 GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
- GC36174 Golotimod 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.
- GC36175 Golotimod (TFA)
- GC38386 Golotimod hydrochloride 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.
- GC33041 Gusacitinib (ASN-002) Gusacitinib (ASN-002) (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 (ASN-002) has anti-cancer activity in both solid and hematological tumor types.
- GC12359 Hispidulin Partial positive allosteric modulator at the benzodiazepine receptor
- GC50343 HJC 0416 hydrochloride STAT3 inhibitor
- GC32807 HJC0152 hydrochloride An orally bioavailable inhibitor of STAT3
- GC16208 HO-3867 STAT3 inhibitor, selective
- GN10742 Homoharringtonine
- GC67958 HP590
- GC33053 HS-10296 hydrochloride Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. HS-10296 hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). HS-10296 hydrochloride is used for the research of the non-small cell lung cancer.
- GC17982 Icotinib EGFR tyrosine kinase inhibitor
- GC64108 Ifidancitinib Ifidancitinib (ATI-50002) is a potent and selective inhibitor of JAK kinases 1/3.
- GC32809 Ilginatinib (NS-018) Ilginatinib (NS-018) (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).
- GC33037 Ilginatinib hydrochloride (NS-018 hydrochloride) Ilginatinib hydrochloride (NS-018 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).
- GC33018 Ilginatinib maleate (NS-018 (maleate)) Ilginatinib maleate (NS-018 (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).
- GC32862 inS3-54A18 inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.
- GC34178 Isocryptotanshinone
- GC19204 Itacitinib Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.
- GC36351 Itacitinib adipate 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.
- GC31866 JAK inhibitor 1 JAK inhibitor 1 is an inhibitor of JAK extracted from patent US20170121327A1, compound example 283.
- GC31999 JAK-IN-1 JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively.
- GC36366 JAK-IN-10 JAK-IN-10 is a JAK inhibitor.
- GC68000 JAK-IN-23
- GC65453 JAK-IN-3 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.
- GC64959 JAK/HDAC-IN-1 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.
- GC33036 JAK1-IN-3 JAK1-IN-3 (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).
- GC33258 JAK1-IN-4 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).
- GC36363 JAK1-IN-7 JAK1-IN-7 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.
- GC36364 JAK2-IN-4 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.
- GC65405 JAK2-IN-6 JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells.
- GC36365 JAK3 covalent inhibitor-1 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.
- GC33046 JAK3-IN-1 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).
- GC31902 JAK3-IN-6 JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.
- GC33382 JAK3-IN-7 JAK3-IN-7 is a potent and selective JAK3 inhibitor extracted from patent WO2011013785A1, has an IC50 of <0.01 μM.
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GC67690
JBJ-09-063 hydrochloride
JBJ-09-063 hydrochloride is a mutation selective allosteric EGFR inhibitor
- GC67860 JBJ-09-063 TFA
- GC65436 JND3229 JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma.
- GC15731 L002 p300 inhibitor
- GC25559 Lapatinib (GW-572016) Ditosylate Lapatinib (GW-572016) Ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
- GC67759 Lapatinib-d4
- GC16021 Lavendustin A EGFR tyrosine kinase inhibitor
- GC19218 Lazertinib Lazertinib is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.
- GC14857 LFM-A13 BTK-specific tyrosine kinase inhibitor
- GC64372 Lorpucitinib Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease.
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GC69410
Lumretuzumab
Lumretuzumab (Anti-Human ERBB3 Recombinant Antibody) is a humanized monoclonal antibody that targets HER3 (ERBB3) and can be used for cancer research.
- GC67706 LY5
- GC34138 M-110 M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
- GC68304 Margetuximab
- GC64710 MC-Val-Cit-PAB-Amide-TLR7 agonist 4 MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a HER2-TLR7 and HER2-TLR8 immune agonist conjugate.
- GC44213 ML115 Signal transducer and activator of transcription 3 (STAT3) is a cytokine-inducible transcription factor with roles in inflammation and cancer.
- GC44227 MM-206 MM-206 is an inhibitor of STAT3 (IC50 = 1.16 μM in an SPR-based competitive assay).
- GC32789 Mogrol 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.
- GC36646 Momelotinib Mesylate 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.
- GN10436 Morusin
- GC19256 MTX-211 MTX-211 is a dual inhibitor of EGFR and PI3K, used for the treatment of cancer and other diseases.
- GC10250 Mubritinib (TAK 165) Mubritinib (TAK 165) (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
- GC11126 Mutant EGFR inhibitor Selective Mutated EGFR inhibitor
- GC36666 Mutated EGFR-IN-1 Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
- GC36667 Mutated EGFR-IN-2 Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity.
- GC11474 Napabucasin STAT3 inhibitor
- GC33022 Naquotinib (ASP8273) Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
- GC32836 Naquotinib mesylate (ASP8273) Naquotinib mesylate (ASP8273) (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
- GC36699 Nazartinib mesylate Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min?1 on EGFR(L858R/790M) mutant, respectively.
- GC66329 NDI-034858 NDI-034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.
- GC10362 Neratinib (HKI-272) Neratinib (HKI-272) (HKI-272) is an orally available, irreversible, highly selective HER2 and EGFR inhibitor with IC50s of 59 nM and 92 nM, respectively.
- GC13586 Niclosamide Inhibitor of the STAT3 signaling pathway
- GC44400 Niclosamide (ethanolamine salt) Niclosamide (BAY2353) olamine is an orally active antihelminthic agent used in parasitic infection research.
- GC15901 Niclosamide monohydrate agent for the treatment of most tapeworm infections