JAK
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1378 | Ruxolitinib (INCB018424) | <1 mg/mL | 61 mg/mL | 61 mg/mL |
| S5001 | Tofacitinib (CP-690550) Citrate | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2162 | AZD1480 | <1 mg/mL | 69 mg/mL | <1 mg/mL |
| S2736 | Fedratinib (SAR302503, TG101348) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S1134 | AT9283 | <1 mg/mL | 76 mg/mL | 38 mg/mL |
| S5243 | Ruxolitinib Phosphate | 29 mg/mL | 80 mg/mL | 8 mg/mL |
| S7812 | Itacitinib (INCB39110) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8541 | FM-381 | <1 mg/mL | 20 mg/mL | 2 mg/mL |
| S2219 | Momelotinib (CYT387) | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2789 | Tofacitinib (CP-690550,Tasocitinib) | <1 mg/mL | 62 mg/mL | <1 mg/mL |
| S2796 | WP1066 | <1 mg/mL | 71 mg/mL | <1 mg/mL |
| S2692 | TG101209 | <1 mg/mL | 102 mg/mL | <1 mg/mL |
| S2179 | Gandotinib (LY2784544) | <1 mg/mL | 94 mg/mL | 9 mg/mL |
| S2686 | NVP-BSK805 2HCl | 3 mg/mL | 113 mg/mL | 15 mg/mL |
| S2851 | Baricitinib (LY3009104, INCB028050) | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2214 | AZ 960 | <1 mg/mL | 71 mg/mL | 3 mg/mL |
| S2806 | CEP-33779 | <1 mg/mL | 36 mg/mL | <1 mg/mL |
| S8057 | Pacritinib (SB1518) | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S2867 | WHI-P154 | <1 mg/mL | 75 mg/mL | <1 mg/mL |
| S7036 | XL019 | <1 mg/mL | 16 mg/mL | <1 mg/mL |
| S2902 | S-Ruxolitinib (INCB018424) | 5 mg/mL | 61 mg/mL | 61 mg/mL |
| S8004 | ZM 39923 HCl | <1 mg/mL | 30 mg/mL | 8 mg/mL |
| S7650 | Peficitinib (ASP015K, JNJ-54781532) | <1 mg/mL | 65 mg/mL | <1 mg/mL |
| S7605 | Filgotinib (GLPG0634) | <1 mg/mL | 85 mg/mL | <1 mg/mL |
| S7541 | Decernotinib (VX-509) | <1 mg/mL | 78 mg/mL | 20 mg/mL |
| S7144 | BMS-911543 | <1 mg/mL | 36 mg/mL | 22 mg/mL |
| S7259 | FLLL32 | <1 mg/mL | 92 mg/mL | 25 mg/mL |
| S2407 | Curcumol | <1 mg/mL | 47 mg/mL | 47 mg/mL |
| S7137 | GLPG0634 analogue | <1 mg/mL | 0.1 mg/mL | <1 mg/mL |
| S8195 | Oclacitinib maleate | 18 mg/mL | 90 mg/mL | 90 mg/mL |
| S7634 | Cerdulatinib (PRT062070, PRT2070) | <1 mg/mL | 43 mg/mL | <1 mg/mL |
| S7119 | Go6976 | <1 mg/mL | 18 mg/mL | <1 mg/mL |
Isoform-specific Inhibitors
- JAK Inhibitors (33)
- New JAK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1378 |
Ruxolitinib (INCB018424)Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. |
a, Phospho- and total STAT1 in MDA-MB-453 cells treated with abemaciclib with or without ruxolitinib for 7 days.
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| S5001 |
Tofacitinib (CP-690550) CitrateTofacitinib citrate (CP-690550 citrate) is a novel inhibitor of JAK with IC50 of 1 nM, 20 nM and 112 nM against JAK3, JAK2, and JAK1, respectively. |
CP-690550 reduced the severity of ischemic damage. (A) CP-690550 (10 μM) suppressed IL-17 production by cdT cells and activated memory T cells. cdT cells and CD4+ CD44+ memory T cells isolated from C5BL6J mice through flow cytometry were stimulated for 24 h with plate-bound monoclonal antibodies to CD3 (2 ng/ml) and CD28 (1 ng/ml) in the presence or absence of IL-23 (25 ng/ml). IL-17A production and IL-17A expression level were measured by quantitative RT-PCR (a) and ELISA (b). (B) CBF reduction after brain ischemia. (C) Time-dependent changes in neurological score. *p < 0.05. (D) Infarct volume as visualized through TTC staining on day 3 in CP-690550 (CP)- and vehicle-treated mice.
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| S2162 |
AZD1480AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM in a cell-free assay, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1. |
bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.
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| S2736 |
Fedratinib (SAR302503, TG101348)Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Phase 2. |
Colony-forming assay results showing that the Jak2 inhibitor TG101348 reduces CFU-GM colonies generated from mutant fetal liver R2 cells. Results from 4 independent control or mutant fetal livers treated with TG101348 or dimethylsulfoxide (DMSO) are shown (mean ?SD). ***P < .001.
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| S1134 |
AT9283AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl(T315I). Phase 2. |
HEL cells were treated with 0.5, 1 or 5 uM of AT9283 or left untreated for 3 hrs. The expression and phosphorylation state of STAT5 (P-STAT5) and Jak2 (P-Jak2) was assessed by Western blot immunodetection.
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| S5243New |
Ruxolitinib PhosphateRuxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. |
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| S7812New |
Itacitinib (INCB39110)Itacitinib(INCB39110) is an orally bioavailable inhibitor of Janus-associated kinase 1 (JAK1) with potential antineoplastic activity. |
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| S8538New |
PF-06651600PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2. |
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| S8541New |
FM-381FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively. |
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| S2219 |
Momelotinib (CYT387)Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3. |
Shown are WT pan T cells (both CD4＋and CD8＋ T cells; CD4－T cells are CD8＋T cells) after drug treatment. |
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| S2789 |
Tofacitinib (CP-690550,Tasocitinib)Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1. |
(J) Western blotting analysis of HIF1α abundance in response to 100 nM tofacitinib. Quantification of HIF1α detected by Western blot is shown alongside, with data normalized to SMC1 intensity and HIF1α protein abundance in IL-2-maintained cytotoxic T lymphocytes.
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| S2796 |
WP1066WP1066 is a novel inhibitor of JAK2 and STAT3 with IC50 of 2.30 μM and 2.43 μM in HEL cells; shows activity to JAK2, STAT3, STAT5, and ERK1/2 not JAK1 and JAK3. Phase 1. |
(A) HRMECs were treated with IL-6 for 48 hours in the presence and the absence of WP1066. The protein expression and localization of ZO-1 was examined by immunofluorescence staining. Each tight junction protein was doubleimmunostained with anti-CD31 antibody for defining the cell boundaries. Nuclei were labeled with DAPI. Arrow heads indicate the intact tight junction protein at cell boundaries. Scale bars are equal to 50 μm. Right histograms: quantitative analysis of each tight junction protein expression by evaluating the fluorescence intensity using with ImageJ software. The results are fold increases versus control and plotted as the means ± SD (n = 5). * P < 0.05 between two values.
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| S2692 |
TG101209TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. |
EGFR-ERCC1 effect on survival. QGP1 cells were transfected with Scrambled, ERCC1, EGFR, or EGFR-ERCC1 siRNA. Following 48 hours of siRNA transfection, Scrambled siRNA and ERCC1 siRNA-transfected cells were treated with 1 umol/L gefitinib or 125 nmol/L NU7026 (DNAPK inhibitor), or both, while EGFR siRNA and EGFR-ERCC1 siRNA-transfected cells were treated with 125 nmol/L of NU7026 1 hour prior 4 Gy IR treatment. Survival of these cells was then assessed 72 hours following IR treatment via MTT assay. The graphs show percentage of survival from 3 independent experiments as compared with untreated control. Bars show SD. Asterisks show statistical significance (*,P < 0.05; **, P < 0.01; ***, P < 0.001; NS, nonsignificant).
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| S2179 |
Gandotinib (LY2784544)Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2. |
Relative expression of BCLXL, c-MYC, CCND1, MMP2 and VEGF in (A) HL60 cell line. Cells were treated with 1 µM of ruxolitinib, fedratinib, gandotinib or tofacitinib for 6 h. RE=1 for DMSO control. Asterix (*) denotes statistical significance (p<0.05). Error bars denotes±standard deviation. Each relative expression value was obtained from at least two biological experiments run in two technical repeats.
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| S2686 |
NVP-BSK805 2HClNVP-BSK805 2HCl is a potent and selective ATP-competitive JAK2 inhibitor with IC50 of 0.5 nM,>20-fold selectivity towards JAK1, JAK3 and TYK2. |
Determination of the kynurenine production in HFF cells after IDO induction by IFN-γ (100 U/mL). The cells were incubated for 72 h under normoxia (20% O2) or hypoxia (1% O2) and treated with different amounts of the JAK2 inhibitor BSK805 (0-2 uM).
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| S2851 |
Baricitinib (LY3009104, INCB028050)Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3. |
bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test. |
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| S2214 |
AZ 960AZ 960 is a novel ATP competitive JAK2 inhibitor with IC50 and Ki of <3 nM and 0.45 nM, 3-fold selectivity of AZ960 for JAK2 over JAK3. |
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| S2806 |
CEP-33779CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2. |
Potentiation of the antitumor effects of vincristine by CEP-33779 in a KBv200 cell xenograft model in nude mice. (A) The changes in tumor volume with time after tumor cell implantation. (B) The photograph of tumor size was taken on the 21st day after implantation. The various treatments were as follows: (a) Control (vehicle alone); (b) Vincristine (q2d x 6, ip, 0.2 mg/kg); (c) CEP-33779 (q2d x 6, p.o, 30 mg/kg) and (d) Vincristine (q2d x 6, ip, 0.2 mg/kg) plus CEP-33779 (q2d ?6, p.o, 30 mg/kg, given an hour before Vincristine administration).
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| S8057 |
Pacritinib (SB1518)Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3. |
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| S2867 |
WHI-P154WHI-P154 is a potent JAK3 inhibitor with IC50 of 1.8 μM, no activity against JAK1 or JAK2, also inhibits EGFR, Src, Abl, VEGFR and MAPK, prevents Stat3, but not Stat5 phosphorylation. |
Reversal effect of WHI-P154 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without WHI-P154. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line. |
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| S7036 |
XL019XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1. |
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| S2902 |
S-Ruxolitinib (INCB018424)S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3. |
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| S8004 |
ZM 39923 HClZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transglutaminase. |
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| S7650 |
Peficitinib (ASP015K, JNJ-54781532)Peficitinib (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3. |
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| S7605 |
Filgotinib (GLPG0634)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. Phase 2. |
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| S7541 |
Decernotinib (VX-509)Decernotinib (VX-509) is a potent and selective JAK3 inhibitor with Ki of 2.5 nM, >4-fold selectivity over JAK1, JAK2, and TYK2, respectively. Phase 2/3. |
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| S7144 |
BMS-911543BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2. |
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| S7259 |
FLLL32FLLL32 is a potent JAK2/STAT3 inhibitor with IC50 of <5 μM. |
Interleukin-6 (IL-6) secretion was inhibited by B7‐H4 silence through JAK2/signal transducer and activator of transcription 3 (STAT3) inactivation. (a) ELISA results showed that, compared with cells pretreated with control shRNA, B7‐H4 silence led to reduction of IL‐6 secretion. However, compared with cells pretreated with control shRNA and FLLL32, IL‐6 secretion in Eca109, TE1, and TE13 esophageal squamous cell carcinoma cells pretreated with B7‐H4 shRNA and FLLL32 was not significantly affected.
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| S2407 |
CurcumolCurcumol is a pure monomer isolated from Rhizoma Curcumaeis with antitumor activities. |
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| S7137 |
GLPG0634 analogueGLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2. |
Western blots showing the expression of γ-globin after treatments with (F) GLPG0634.
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| S8195 |
Oclacitinib maleateOclacitinib(PF 03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM. It does not inhibit a panel of 38 non-JAK kinases. |
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| S7634 |
Cerdulatinib (PRT062070, PRT2070)Cerdulatinib (PRT-062070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM. |
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| S7119 |
Go6976Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3. |
Erk5 activation depends on Mek5, classical PKC and Mek1/2. MOVAS cells were serum-starved overnight and then treated for 1 h if not indicated otherwise with inhibitors targeting Jnk (SP600125, 10 μM), p38 (SB203580, 10 μM), Mek1/2 (CI-1040, 3 μM), Jak2 (AG490, 10 μM), Src (SU6656, 0.5 μM), Go6983 (PKC, 1 μM), Gö6976 (classical PKC, 1 μM), proteasomes (MG132, 25 μM), TPA (100 ng/ml for 15 min to activate PKCs or overnight to inhibit) and Mek5 (BIX02189, 1 μM), as well as Ca2 + chelators (EDTA, 2 mM; BAPTA-AM, 10 μM; both with 30 min preincubation), followed by stimulation with 20 ng/ml PDGF-BB for 10 min. Total cell lysates (TCL) were prepared and subjected to SDS-PAGE. Erk5 and PDGFRβ activities were measured by band shift and Tyr857 phosphorylation, respectively, using immunoblotting. Panel E and G show representative immunoblots. |
