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Catalog No.
Product Name
Application
Product Information
Product Citation
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EGFR inhibitor
AG 490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.- Matozaki M, .et al. , Exp Cell Res, 2019, Feb 15. pii: S0014-4827(18)31030-9 PMID: 30776355
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JAK Inhibitor
AZD1480 is a novel potent small JAK2 inhibitor with an IC50 of 0.26 nM.- Simona Moravcova, .et al. , Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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JAK3 inhibitor
CP-690550 (Tofacitinib citrate) is an orally available, highly selective inhibitor of the Janus kinase (JAK) family of enzymes.- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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JAK inhibitor
CYT387 is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively.- Alex Bainbridge, .et al. , Nucleic Acids Research, 2020, April
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JAK inhibitor
LY2784544 is identified as being highly selective for JAK2-V617F and has advanced into human clinical trials for the treatment of several myeloproliferative disorders. -
JAK1/2 Inhibitor
INCB018424 is a potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively;- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. , Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. , Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
JAK inhibitor
BMS-911543 is an orally available small molecule targeting a subset of Janus-associated kinase (JAK) with potential antineoplastic activity. -
JAK Inhibitor
Baricitinib, also known as INCB028050 or LY3009104, is a selective orally bioavailable JAK1/JAK2 inhibitor with nanomolar potency against JAK1 (5.9 nM) and JAK2 (5.7 nM).- Dandan Wang, .et al. , Adv Rheumatol, 2023, May 16;63(1):22 PMID: 37194022
- Yuki Sasaki, .et al. , JCI Insight, 2022, Apr 8;7(7) PMID: 35393946
- Yutian Lei, .et al. , Kidney Int, 2021, Feb 16 PMID: 33607177
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JAK1/2 inhibitor
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. -
JAK inhibitor
Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. -
JAK Inhibitor
WP1066 is a novel JAK2 inhibitor and it suppresses proliferation and induces apoptosis in eythroid human cells carrying the JAK2 V617F mutation.- Simona Moravcova, .et al. , Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor. -
JAK2/FLT3 inhibitor
Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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JAK1 inhibitor
PF-03394197 (oclacitinib) is a potent JAK1 inhibitor- Steven E. Davison, .et al. , PLoS One, 2022, Oct 18;17(10):e0276333 PMID: 36256616
- Banovic F, .et al. , Vet Dermatol, 2018, Nov 12 PMID: 30417482
- Nicholas B, .et al. , J Allergy Clin Immunol, 2017, Jul;140(1):309-312.e4 PMID: 28259448
- Fukuyama T, .et al. , J Pharmacol Exp Ther., 2015, Sep;354(3):394-405 PMID: 26159873
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JAK3 inhibitor
ZM 39923 HCl is an inhibitor of JAK3 (IC50 = 79 nM) that less potently inhibits epidermal growth factor receptor, JAK1, and cyclin-dependent kinase 4 (IC50s = 2.4, 40, and 10 M, respectively) -
JAK3 inhibitor
Decernotinib is an oral, selective Janus kinase 3 (JAK3) inhibitor being developed by Vertex. -
JAK2 inhibitor
Z3 is a novel specific inhibitor of Jak2 tyrosine kinase. -
multi-targeted tyrosine kinase inhibitor
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. -
JAK inhibitor
Filgotinib is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. -
JAK inhibitor
Peficitinib is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats. -
JAK inhibitor
S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor. -
JAK inhibitor
Baricitinib phosphate is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. -
JAK2 inhibitor
1,2,3,4,5,6-Hexabromocyclohexane is a potent and specific inhibitor of JAK2 autophosphorylation. -
JAK2/STAT3 inhibitor
Cucurbitacin I, Cucumis sativus L. has been found to suppress levels of phosphotyrosine Stat3 (signal transducer and activator of transcription 3) in v-Src-transformed NIH 3T3 cells. -
JAK inhibitor
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).- Carlos H de Mello Souza, .et al. , Vet Dermatol, 2021, Dec 9 PMID: 34882871
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JAK3 inhibitor
PF-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. -
JAK3/2/1 inhibitor
Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
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JAK1 Inhibitor
Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM. IC50 & Target: IC50: 43 nM (JAK1), 200 nM (JAK2) -
JAK3 inhibitor
JAK3-IN-2 is a potent and highly selective JAK3 inhibitor with IC50 of 0.15 nM. dispalys >4,300-fold selectivity over JAK1, JAK2 and TYK2, and other kinases BMX, EGFR, ITK and BTK; blocks cytokine signaling through JAK3, but not through other JAK family enzymes; inhibits IL-7 induced pSTAT5 in CD3+, CD8+ T cells with IC50 of 280 nM; sufficiently blocks the development of inflammation in a rat model of rheumatoid arthritis, while sparing hematopoiesis. -
dual JAK1/TYK2 inhibitor
PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively.
