Catalog No.
Product Name
Application
Product Information
Citations
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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.- Angelina T Regua, .et al. , Cancer Lett, 2024, Jun 7:597:217023 PMID: 38852701
- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
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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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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.- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Alex Bainbridge, .et al. , Nucleic Acids Research, 2020, April PMID: 32324216
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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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JAK1 Inhibitor
INCB39110 is a potent JAK1 tyrosine kinase inhibitor, which is currently in Phase II trials for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis.- Czech J, .et al. , Leukemia, 2018, Nov 23 PMID: 30470838
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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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JAK1/JAK2 inhibitor
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.- Ghazal Nabil, .et al. , Cancers (Basel), 2021, Feb 20;13(4):898 PMID: 33672756
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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).- Haruka Nishimura, .et al. , J Med Invest, 2025, 72(3.4):298-307 PMID: 41183930
- Lokesh Sharma, .et al. , Physiol Rep, 2025, Feb;13(3):e70232 PMID: 39921246
- Renlei Feng, .et al. , BMC Cardiovasc Disord, 2025, Jan 31;25(1):65 PMID: 39891042
- Hongli Liu, .et al. , Adv Rheumatol, 2023, Aug 28;63(1):45 PMID: 37641106
- 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/JAK2 Inhibitor
AZD1480 is a novel potent small JAK2 inhibitor with an IC50 of 0.26 nM.- Jacob W Feldmann, .et al. , The Journal of Immunology, 2025, Nov 25 PMID: 41290006
- Simona Moravcova, .et al. , Life (Basel), 2021, Oct 18;11(10):1105 PMID: 34685476
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JAK1 inhibitor
GLPG0634 is an orally-available, selective inhibitor of JAK1 (Janus kinase 1) being developed by Galapagos for the treatment of rheumatoid arthritis and potentially other inflammatory diseases.- Keisuke Nishimura, .et al. , Arthritis Rheumatol., 2015, Apr;67(4):893-902 PMID: 25545152
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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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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;- Meenu Kesarwani, .et al. , Blood Adv, 2024, Jun 11;8(11):2765-2776 PMID: 38531054
- 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 inhibitor
AZ-960 is a potent, selective and ATP competitive JAK2 inhibitor that inhibits JAK2 kinase with a Ki of 0.45 nM in vitro and induces growth arrest and apoptosis in adult T-cell leukemia (ATL) cell.- Rongshou Wu, .et al. , Sci Rep, 2023, 13: 16998 PMID: 37813900
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JAK2 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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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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Aurora/JAK inhibitor
AT9283 inhibits aurora kinase A and B and targets other tyrosine and serine/threonine kinases associated with myeloid cell proliferation.- Tomoya Takeda, .et al. , Oncol Rep, 2020, August 18 PMID: 33000229
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JAK inhibitor
JAK Inhibitor I is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK1, JAK2, and JAK3.- Ya-Ge Zhang, .et al. , J Neuroinflammation, 2023, Sep 27;20(1):216 PMID: 37752509
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JAK3 Inhibitor
JAK3-IN-13 is a selective and orally bioavailable inhibitor of JAK3, exhibiting IC50 values of 4728, 2039, 8, and 365 nM against NK1, JNK2, JNK3, and Tyk2, respectively. This compound demonstrates significant antiproliferative effects and induces cell cycle arrest in the G0/G1 phase. JAK3-IN-13 is particularly relevant for research applications focused on tumor biology and the modulation of immune responses. -
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. -
JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
JAK2/3 PROTAC Degrader
SJ10542 is a potent and selective PROTAC degrader targeting JAK2 and JAK3. With DC50 values of 14 nM for JAK2 and 11 nM for JAK3 in patient-derived xenograft cells (PDX), SJ10542 demonstrates significant antitumor activity. This compound is valuable for research in hematological malignancies and autoimmune diseases, facilitating the exploration of targeted degradation mechanisms in these therapeutic areas. -
PROTAC JAK2 Degrader
SJ988497 is a potent PROTAC JAK2 degrader that targets JAK2 for degradation, playing a critical role in the inhibition of CRLF2-rearranged (CRLF2r) cell proliferation. Functionally, SJ988497 induces degradation of the neosubstrate GSPT1 through its architecture consisting of a Ruxolitinib derivative, a linker, and the CRBN ligand Pomalidomide. This compound is particularly valuable for research focused on acute lymphoblastic leukemia (ALL). -
JAK1 PROTAC Degrader
PROTAC JAK1 Degrader 1 is a selective PROTAC agent targeting JAK1, exhibiting a DC50 of 214 nM. This compound initiates rapid degradation of JAK1, leading to significant antitumor activity. It serves as a valuable tool for investigating JAK1-related signaling pathways and developing therapeutic strategies for malignancies driven by JAK1 dysregulation. -
TYK2 Degrader
PROTAC TYK2 degradation agent1 is a selective degrader targeting TYK2, effectively facilitating its degradation with a DC50 value of 14 nM. This compound highlights significant biological activity in modulating TYK2 levels, making it a useful tool for investigating autoimmune diseases. Research applications include studying the role of TYK2 in inflammatory pathways and evaluating potential therapeutic strategies. -
PTPN1/PTPN2 Inhibitor
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction. -
JAK-STAT Inhibitor
WP-1034 is a selective JAK-STAT inhibitor that exhibits pro-apoptotic and antileukemic properties, particularly in acute myeloid leukemia (AML) models. By blocking the activation of Stat 3 and Stat 5, WP-1034 effectively induces cell cycle arrest and triggers apoptosis in affected cells. This reagent is valuable for research focused on understanding the mechanisms and therapeutic avenues in AML. - 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
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JAK2/FLT3 inhibitor
Flonoltinib is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM for JAK2, 4 nM for FLT3, 26 nM for JAK1, and 39 nM for JAK3. It exhibits strong anti-cancer activity and is a promising candidate for the treatment of hematologic malignancies and other JAK/FLT3-driven cancers. -
PROTAC JAK2 Degrader
SJ1008030 (compound 8) TFA is a selective JAK2-targeting PROTAC that promotes proteasomal degradation of Janus kinase 2 (JAK2). It exhibits potent antiproliferative activity in MHH–CALL-4 leukemia cells, with an IC₅₀ of 5.4 nM. By effectively eliminating JAK2 protein rather than merely inhibiting its activity, SJ1008030 TFA represents a promising therapeutic strategy for JAK2-driven hematologic malignancies, particularly in leukemia research. -
Aurora Kinase A/JAK2 Inhibitor
AJI-214 is a dual-target inhibitor that simultaneously inhibits Aurora kinase A and Janus kinase 2 (JAK2). It directly blocks Aurora A activity, disrupting T cell mitotic progression and polarity, while also inhibiting JAK2-mediated STAT3 phosphorylation, thereby suppressing the differentiation of pro-inflammatory TH1 and TH17 cells. AJI-214 holds therapeutic potential for modulating immune responses and is being investigated for the prevention and treatment of graft-versus-host disease (GVHD). -
PROTAC JAK2 degrader
SJ1008030 (Compound 8) formic is a selective PROTAC degrader of JAK2, designed to target and eliminate JAK2 protein via the ubiquitin–proteasome pathway. It effectively inhibits the growth of MHH–CALL-4 leukemia cells with an IC₅₀ of 5.4 nM. SJ1008030 formic is a valuable tool for leukemia research and the study of JAK2-driven signaling pathways. -
JAK2 Inhibitor
Itacnosertib is a selective inhibitor of JAK2, with an IC50 value of 8540 nM, and it also targets FLT3 and ACVR1 (ALK2) with an IC50 of 8 nM. This compound demonstrates significant anti-leukemic activity, making it valuable for research in hematological malignancies. Itacnosertib is utilized in studies investigating the mechanisms of JAK2-mediated signaling pathways and the development of targeted therapies for related disorders. -
JAK Inhibitor
JAK-IN-39 is a potent inhibitor of the Janus kinase (JAK) family, specifically targeting JAK1, JAK2, and JAK3 with IC50 values of 0.05, 1.18, and 0.03 nM, respectively. This compound effectively reduces the viability of TF-1 cells and inhibits the production of pro-inflammatory cytokines, including TNFα and IFNγ, in vitro. JAK-IN-39 is valuable for research into immune regulation and potential therapeutic applications in inflammatory diseases and hematological malignancies. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-3 is a dual inhibitor targeting Janus kinase (JAK) and histone deacetylases (HDAC). It exhibits potent inhibitory activity with IC50 values of 25.36 nM for JAK2, and 0.2 μM and 0.43 μM for HDAC and HDAC1, respectively. This compound is valuable for investigating the roles of JAK and HDAC pathways in cellular processes and disease models, particularly in cancer and inflammatory research. -
JAK3 Inhibitor
DPPY is a potent JAK3 inhibitor with an IC50 of less than 10 nM, demonstrating high selectivity for protein tyrosine kinases including EGFR and BTK. It exhibits significant anti-proliferative activity against B-cell lymphoma cells. DPPY holds potential for research applications related to idiopathic pulmonary fibrosis (IPF) and other conditions involving aberrant JAK3 signaling. -
JAK Inhibitor
MJ04 is a selective inhibitor targeting Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. This compound effectively inhibits T cell differentiation and reduces pro-inflammatory cytokine production in lipopolysaccharide-induced macrophages. Additionally, MJ04 exhibits favorable pharmacokinetic properties in mice and has demonstrated the ability to promote hair growth in a dihydrotestosterone-induced model of androgenetic alopecia (AGA), showing minimal toxicity (LD50 > 2 g/kg). -
pan-JAK inhibitor
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. -
JAK2/HDAC dual inhibitor
JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. -
JAK inhibitor
NVP-BSK805 is a potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor that potently suppressed recombinant human erythropoietin-induced polycythemia and extramedullary erythropoiesis in mice and rats.
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JAK inhibitor
BMS-911543 is an orally available small molecule targeting a subset of Janus-associated kinase (JAK) with potential antineoplastic activity. -
multi-kinase inhibitor
Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively. -
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. -
FLT3 inhibitor
TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.
