JAK/STAT Signaling Pathway Inhibitors

The Janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway is a critical signaling cascade for mediating cytokine receptor-derived signals. JAK/STAT signaling contributes to the regulation of haematopoietic cell survival, proliferation and differentiation. Also, this signaling pathway is involved in the developmental process, growth regulation and maintenance of homeostasis in other cells and tissues. The JAK/STAT signaling pathway is made up of four JAKs (JAK1-3, and Tyk2) and seven STAT proteins (STAT1-4, 5A, 5B and 6).

Initiation of JAK/STAT signaling proceeds as a result of cytokine receptors activating a specific set of individual JAKs and STATs that is dependent on the characteristics of the intracellular domains of the receptor chains. The binding of cytokines to transmembrane receptors (i.e. interleukin-2 or interferon) results in cross-activation of receptor-associated JAKs by tyrosine phosphorylation due to receptor dimerization and reorganization events. Activated JAKs lead to the phosphorylation of tyrosine residues in the cytoplasmic domain that increases their catalytic activity for STAT proteins. JAKs mediate phosphorylation on the C-terminus. This in turn causes STAT proteins to dissociate from the receptor, dimerize (mediated by Src-homology-2 domains) and translocate to the cell nucleus where they induce gene transcription of intracellular regulators of cell proliferation (cyclins and Myc) and survival (Bcl family). Regulating the JAK/STAT signaling pathway are SOCS1, SOCS3 and PIAS3. Constitutive signaling of the JAK/STAT pathway, high levels of STAT3 proteins and/or deminished function of negative regulators can contribute to tumour initiation and progression events.

Cat. No.DescriptionProduct groups

JAK inhibitors

S1143AG-490 (Tyrphostin B42) (CAS no: 133550-30-8)Chemicals
S1134AT9283 (CAS no: 896466-04-9)Chemicals
S2214AZ 960 (CAS no: 905586-69-8)Chemicals
S2162AZD1480 (CAS no: 935666-88-9)Chemicals
S2851Baricitinib (LY3009104, INCB028050) (CAS no: 1187594-09-7)Chemicals
S2806CEP-33779 (CAS no: 1257704-57-6)Chemicals
S7634Cerdulatinib (PRT062070, PRT2070) [CAS no: 1369761-01-2]Chemicals
S2407Curcumol (CAS no: 4871-97-0)Chemicals
S2219CYT387 (CAS no: 1056634-68-4)Chemicals
S7541Decernotinib (VX-509) [CAS no: 944842-54-0]Chemicals
S7605Filgotinib (GLPG0634)(CAS no: 1206161-97-8)Chemicals
S7259FLLL32 [CAS no: 1226895-15-3]Chemicals
S7119Go6976 [CAS no: 136194-77-9]Chemicals
S2179LY2784544 (CAS no: 1229236-86-5)Chemicals
S2686NVP-BSK805 2HCl (CAS no: 1092499-93-8)Chemicals
S8057Pacritinib (SB1518) (CAS no: 937272-79-2)Chemicals
S7650Peficitinb (ASP015K, JNJ-54781532) [CAS no: 944118-01-8]Chemicals
S1378Ruxolitinib (INCB018424) (CAS no: 941678-49-5)Chemicals
S2902S-Ruxolitinib (INCB018424) (CAS no: 941685-37-6)Chemicals
S2692TG101209 (CAS no: 936091-14-4)Chemicals
S2736TG101348 (SAR302503) (CAS no: 936091-26-8)Chemicals
S5001Tofacitinib (CP-690550) Citrate (CAS no: 540737-29-9)Chemicals
S2789Tofacitinib (CP-690550,Tasocitinib) (CAS no: 477600-75-2)Chemicals
S2867WHI-P154 (CAS no: 211555-04-3)Chemicals
S2796WP1066 (CAS no: 857064-38-1)Chemicals
S7036XL019 (CAS no: 945755-56-6)Chemicals
S8004ZM 39923 HCl (CAS no: 1021868-92-7)Chemicals

STAT inhibitors

S2285Cryptotanshinone (CAS no: 35825-57-1)Chemicals
S1491Fludarabine (CAS no: 21679-14-1)Chemicals
S7501HO-3867 [CAS no: 1172133-28-6]Chemicals
S7977Napabucasin [CAS no: 83280-65-3]Chemicals
S3030Niclosamide (CAS no: 50-65-7)Chemicals
S4182Nifuroxazide (CAS no: 965-52-6)Chemicals
S1155S3I-201 (CAS no: 501919-59-1)Chemicals
S7337SH-4-54 [CAS no: 1456632-40-8]Chemicals
S7024Stattic (CAS no: 19983-44-9)Chemicals

EGFR inhibitors

S1056AC480 (BMS-599626) (CAS no: 714971-09-2)Chemicals
S1486AEE788 (NVP-AEE788) (CAS no: 497839-62-0)Chemicals
S1011Afatinib (BIBW2992) (CAS no: 439081-18-2)Chemicals
S7810Afatinib (BIBW2992) Dimaleate [CAS no: 850140-73-7]Chemicals
S2728AG-1478 (Tyrphostin AG-1478) (CAS no: 153436-53-4)Chemicals
S8009AG-18 (CAS no: 118409-57-7)Chemicals
S1143AG-490 (Tyrphostin B42) (CAS no: 133550-30-8)Chemicals
S2185AST-1306 (CAS no: 1050500-29-2)Chemicals
S7298AZ5104 [CAS no: 1421373-98-9]Chemicals
S7971AZD3759 [CAS no: 1626387-80-1]Chemicals
S2192AZD8931 (Sapitinib) (CAS no: 848942-61-0)Chemicals
S8036Butein (CAS no: 487-52-5)Chemicals
S1019Canertinib (CI-1033) (CAS no: 267243-28-7)Chemicals
S2406Chrysophanic Acid (CAS no: 481-74-3)Chemicals
S7557CL-387785 (EKI-785) [CAS no: 194423-06-8]Chemicals
S7206CNX-2006 (CAS no: 1375465-09-0)Chemicals
S7284CO-1686 (AVL-301) (CAS no: 1374640-70-6)Chemicals
S1167CP-724714 (CAS no: 537705-08-1)Chemicals
S1194CUDC-101 (CAS no: 1012054-59-9)Chemicals
S2727Dacomitinib (PF299804, PF299) (CAS no: 1110813-31-4)Chemicals
S2554Daphnetin (CAS no: 486-35-1)Chemicals
S7786Erlotinib (CAS no: 183321-74-6)Chemicals
S1023Erlotinib HCl (OSI-744) (CAS no: 183319-69-9)Chemicals
S1025Gefitinib (ZD1839) (CAS no: 184475-35-2)Chemicals
S1342Genistein (CAS no: 446-72-0)Chemicals
S2922Icotinib (CAS no: 610798-31-7)Chemicals
S2111Lapatinib (CAS no: 231277-92-2)Chemicals
S1028Lapatinib (GW-572016) Ditosylate (CAS no: 388082-77-7)Chemicals
S2150Neratinib (HKI-272) (CAS no: 698387-09-6)Chemicals
S2205OSI-420 (CAS no: 183320-51-6)Chemicals
S7297Osimertinib (AZD9291) [CAS no: 1421373-65-0]Chemicals
S1079PD153035 HCl (CAS no: 183322-45-4)Chemicals
S7039PD168393 (CAS no: 194423-15-9)Chemicals
S1392Pelitinib (EKB-569) (CAS no: 257933-82-7)Chemicals
S7358Poziotinib (HM781-36B) [CAS no: 1092364-38-9]Chemicals
S2784TAK-285 (CAS no: 871026-44-7)Chemicals
S2895Tyrphostin 9 (CAS no: 10537-47-0)Chemicals
S2755Varlitinib (CAS no: 845272-21-1)Chemicals
S2867WHI-P154 (CAS no: 211555-04-3)Chemicals
S1170WZ3146 (CAS no: 1214265-56-1)Chemicals
S1173WZ4002 (CAS no: 1213269-23-8)Chemicals
S1179WZ8040 (CAS no: 1214265-57-2)Chemicals

Pim inhibitors

S7104AZD1208 [CAS no: 1204144-28-4]Chemicals
S7041CX-6258 HCl [CAS no: 1353859-00-3]Chemicals
S2198SGI-1776 free base (CAS no: 1025065-69-3)Chemicals
S8005SMI-4a (CAS no: 438190-29-5)Chemicals

Related to:
Brands: Selleck Chemicals
Product groups: Chemicals​