Targets for JAK/STAT Signaling
Products for JAK/STAT Signaling
- Cat.No. Product Name Information
- GC38006 β-Hydroxyisovalerylshikonin Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
- GC34964 (1S,3R,5R)-PIM447 dihydrochloride (1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
- GC34971 (3R,4S)-Tofacitinib (3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib.
- GC34972 (3S,4R)-Tofacitinib (3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib.
- GC34973 (3S,4S)-Tofacitinib (3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib.
- GC61807 (E/Z)-AG490 (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
- GC63864 (E/Z)-Zotiraciclib hydrochloride (E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor.
(R,R)-VVD-118313 is an isomer of VVD-118313. VVD-118313 is a selective JAK1 inhibitor that can block JAK1-dependent phosphorylation and cytokine signaling. VVD-118313 can be used for cancer research.
- GC63797 (S)-Sunvozertinib (S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK.
- GC46503 2-(1,8-Naphthyridin-2-yl)phenol 2-(1,8-Naphthyridin-2-yl)phenol is a selective enhancer of STAT1 transcription. 2-(1,8-Naphthyridin-2-yl)phenol can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells.
- GC12138 5,15-DPP 5,15-DPP (5,15-DPP) is a selective STAT3-SH2 antagonist (IC50s of 0.28 μM and 10 μM for STAT3 and STAT1, respectively).
- GC32023 Abrocitinib (PF-04965842) Abrocitinib (PF-04965842) (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively.
- GC62272 AC-4-130 AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).
- GC13257 AC480 (BMS-599626) AC480 (BMS-599626) (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. AC480 (BMS-599626) displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. AC480 (BMS-599626) inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
- GC11892 AEE788 (NVP-AEE788) AEE788 (NVP-AEE788) is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
- GC11744 AG 555 Potent EGFR-kinase inhibitor
- GC13168 AG 825 Selective ErbB2 inhibitor
- GC14494 AG 99 AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
- GC17226 AG-1478 EGFR inhibitor,potent and selective
- GC12864 AG-1557 inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase
- GC17647 AG-18 AG-18 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.
- GC13854 AG-490 (Tyrphostin B42) AG-490 (Tyrphostin B42) (Tyrphostin AG-490 (Tyrphostin B42)) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
- GN10705 Alantolactone
- GC64398 Almonertinib mesylate Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate 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). Almonertinib mesylate is used for the research of the non-small cell lung cancer.
- GC67749 Amivantamab
- GC60585 Angoline Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
- GC60586 Angoline hydrochloride Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
- GC17283 AP26113 AP26113 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
- GC10439 APTSTAT3-9R STAT3 inhibitor
- GC35395 Arnicolide D 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.
- GC12478 ARRY-380 ARRY-380, an inhibitor of EGFR (ErbB1), is extracted from patent WO2015153959A2, compound 249. ARRY-380 is a potent, selective, ATP-competitive, orally active inhibitor of HER2.
- GC10889 Artesunate Derivative of the natural product artemisinin
- GC19039 AS1517499 A potent STAT6 inhibitor
- GC61574 AS1810722 AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM.
- GC38736 AS2863619 A dual inhibitor of Cdk8 and Cdk19
- GC38737 AS2863619 free base 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.
- GC40715 Ascochlorin Ascochlorin is an isoprenoid antibiotic and antiviral that has diverse effects on mammalian cells.
- GC11691 AST-1306 AST-1306 (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. AST-1306 also inhibits ErbB4 with an IC50 of 0.8 nM. AST-1306 is an anilino-quinazoline compound and has anti-cancer activity.
- GC15669 AST-1306 TsOH AST-1306 TsOH (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. AST-1306 TsOH also inhibits ErbB4 with an IC50 of 0.8 nM. AST-1306 TsOH is an anilino-quinazoline compound and has anti-cancer activity
- GC33096 AST2818 mesylate Alflutinib (Furmonertinib) mesylate is is a potent inhibitor of EGFR. Alflutinib (Furmonertinib) mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Alflutinib (Furmonertinib) mesylate has the potential for the research of cancer diseases, especially non-small cell lung cancer (NSCLC).
- GC35413 Astragaloside VI Astragaloside VI could activate EGFR/ERK signalling pathway to improve wound healing.
- GN10627 Atractylenolide I
- GC35435 AV-412 A dual inhibitor of EGFR and HER2
- GC35436 AV-412 free base AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
A pyrrolopyrimidine-based irreversible EGFR inhibitor
- GC12955 AZ5104 EGFR inhibitor
- GC16308 AZD-9291 AZD-9291 (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. AZD-9291 overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
- GC16698 AZD-9291 mesylate AZD-9291 mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.
- GC35447 AZD1208 hydrochloride AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
- GC13143 AZD3759 AZD3759 (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively.
- GC13761 AZD8931 (Sapitinib) AZD8931 (Sapitinib) (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
- GC18126 Balsalazide anti-inflammatory drug
- GC35466 Balsalazide sodium hydrate Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
- GC64302 BAY 2476568 BAY 2476568 is a potent and selective EGFR inhibitor, with IC50s of < 0.2 nM for wild-type EGFR and several mutations (EGFRR ex20insSVD, EGFRR ex20insASV, EGFRR ex20insNPG).
- GC64017 Befotertinib Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).
- GC33172 BGB-102 (JNJ-26483327) BGB-102 (JNJ-26483327) is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
- GC19066 BGB-283 BGB-283 is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.
- GC38402 BI-4020 A fourth-generation and non-covalent EGFR tyrosine kinase inhibitor
- GC63910 BLU-945 BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC).
- GC32028 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
- GC34063 BP-1-102 A STAT3 inhibitor
- GC42974 Brassinin Brassinin (BSN) is a phytoalexin isolated from B.
- GC25168 Brepocitinib (PF-06700841) Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
- GC35554 Brevilin A A sesquiterpene lactone with anticancer activity
- GC10944 Butein Protein kinase inhibitor
- GC34076 C188-9 A STAT3 inhibitor
- GC12910 Canertinib (CI-1033) Canertinib (CI-1033) (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM.
- GC47061 CAY10763 A dual inhibitor of IDO1 and STAT3 activation
- GC49139 CAY10784 A STAT3 inhibitor
- GC35651 Cenisertib Cenisertib (AS-703569) is an ATP-competitive 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.
- GC11209 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070) (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
- GC34217 Cetuximab (C225) Cetuximab (C225) (C225) is a human IgG1 monoclonal antibody that inhibits epidermal growth factor receptor (EGFR), with a Kd of 0.201 nM for EGFR by SPR. Cetuximab (C225) has potent antitumor activity.
- GC15950 CGP 52411 EGFR inhibitor
- GC25219 CH7233163 CH7233163 is a non-covalent ATP competitive inhibitor of EGFR-tyrosine kinase with antitumor activities against tumor with EGFR-Del19/T790M/C797S.
- GC35684 CHMFL-EGFR-202 CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ?10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
- GC11652 CHZ868 Type II JAK2 inhibitor
- GC17790 CL-387785 (EKI-785) CL-387785 (EKI-785)(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR with IC50 of 370 pM.
- GC34238 CMD178 CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development.
- GC35715 CMD178 TFA CMD178 TFA is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development.
mutant-EGFR inhibitor, selective and irreversible
- GC14854 Colivelin Colivelin (CLN) is A brain-permeable neuroprotective peptide.
- GC35720 Colivelin TFA Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3?in vitro.
- GC13279 Corylifol A STAT3 inhibitor
- GC13091 CP-724714 HER2 inhibitor,potent and selective
- GN10501 Cryptotanshinone
- GC13347 Cucurbitacin I An inhibitor STAT3/JAK signaling
- GN10442 Curculigoside
- GC35762 CX-6258 hydrochloride hydrate CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
- GC38180 Cyasterone
- GC10225 Dacomitinib (PF299804, PF299) Dacomitinib (PF299804, PF299) (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
- GC65020 Danvatirsen Danvatirsen is an antisense oligonucleotide targeting STAT3 with potential antitumor activity. Danvatirsen binds to STAT3 mRNA, thereby inhibiting translation of the transcript. Suppression of STAT3 expression induces tumor cell apoptosis and decreases tumor cell growth.
- GC31660 Delgocitinib (JTE-052) Delgocitinib (JTE-052) (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.
Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which serves as the precursor of certain anthocyanins that provide the blue-red colors of flowers, fruits, and red wine.
- GC34101 Dihydroisotanshinone I
- GN10115 Diosgenin
- GC64039 Disitamab vedotin Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent Monomethyl auristatin E (MMAE). Disitamab vedotin enhances antitumor immunity.
- GC66432 EAI001 EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer.
- GC12281 EAI045 Inhibitor of L858R/T790M EGFR mutants
- GC16321 EGF816 EGF816 (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min-1 on EGFR(L858R/790M) mutant, respectively.
- GC35965 EGFR mutant-IN-1 EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM).