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Tyrosine Kinases

A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to a protein in a cell. It functions as an "on" or "off" switch in many cellular functions. Tyrosine kinases are a subclass of protein kinase.The phosphate group is attached to the amino acid tyrosine on the protein. Tyrosine kinases are a subgroup of the larger class of protein kinases that attach phosphate groups to other amino acids (serine and threonine). Phosphorylation of proteins by kinases is an important mechanism in communicating signals within a cell (signal transduction) and regulating cellular activity, such as cell division.

  • Ruxolitinib
    T1829941678-49-5
    Ruxolitinib (INCB018424) is a JAK1 2 inhibitor (IC50=3.3 2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
    • $53
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  • Delgocitinib
    T150961263774-59-9
    Delgocitinib (JTE-052) is a specific JAK (Janus kinase) inhibitor with IC50 values of 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2 respectively. Delgocitinib is involved in various inflammatory and autoimmune diseases through JAK-dependent cytokines and can effectively suppress multiple cytokine signaling while inhibiting itching caused by cytokines. It is widely used to treat various inflammatory diseases, including autoimmune diseases and hypersensitivity reactions.
    • $172
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  • Zongertinib
    T695342728667-27-2In house
    Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.
    • $148
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  • Deucravacitinib
    T146871609392-27-9
    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable, allosteric TYK2 inhibitor for the treatment of autoimmune diseases. It blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain, inhibiting IL-12 23 and type I IFN pathways. It selectively binds to the TYK2 pseudokinase (JH2) domain with an IC50 of 1.0 nM.
    • $64
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  • Hypericin
    T6S0923548-04-9
    Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.
    • $52
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  • Ibrutinib
    T1835936563-96-1
    Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
    • $36
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  • Gefitinib
    T1181184475-35-2
    Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.
    • $50
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  • Baricitinib
    T24851187594-09-7
    Baricitinib (INCB028050) is a JAK1 and JAK2 inhibitor (IC50=5.9 5.7 nM) with selective and oral activity. Baricitinib has potential anti-inflammatory, immunomodulatory and anti-tumor activity.
    • $43
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  • Lorlatinib
    T30611454846-35-5
    Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
    • $35
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  • Pacritinib
    T6020937272-79-2
    Pacritinib (SB1518) (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
    • $34
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  • Ropsacitinib
    T13237L2127109-84-4
    Ropsacitinib (PF-06826647) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain (IC50: 17 nM).
    • $243
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  • Decernotinib
    T2636944842-54-0
    Decernotinib (VRT-831509)(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
    • $44
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  • Peficitinib
    T6933944118-01-8
    Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.
    • $38
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  • TAK-659 hydrochloride
    T42091952251-28-3
    TAK-659 hydrochloride (TAK-659) is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
    • $33
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  • Beta-Hydroxyisovalerylshikonin
    TN14407415-78-3
    Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).
    • $139
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  • Filgotinib
    T19291206161-97-8
    Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 values of 10 nM for JAK1, 28 nM for JAK2, 810 nM for JAK3, and 116 nM for TYK2.
    • $33
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  • Alectinib
    T19361256580-46-7
    Alectinib (RG-7853) is an ALK inhibitor (IC50=1.9 nM, Kd=2.4 nM) that is selective, orally active, and ATP-competitive. Alectinib has antitumor activity and is used in the treatment of non-small cell lung cancer.
    • $39
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  • Geldanamycin
    T634330562-34-6
    Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR) HSP association.
    • $39
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  • Ilginatinib
    T122661239358-86-1
    Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor.
    • $58
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  • Pyridone 6
    T3080457081-03-7
    Pyridone 6 (JAK Inhibitor)(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
    • $75
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  • Oclacitinib maleate
    T69141640292-55-2
    Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members, with IC50 values ranging from 10 to 99 nM, and JAK1-dependent cytokines, with IC50 ranging from 36 to 249 nM, while not inhibiting a panel of 38 non-JAK kinases.
    • $33
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  • Larotinib
    T733341438072-11-7
    Larotinib is an orally active, potent, and broad-spectrum tyrosine kinase inhibitor (TKI) with an IC50 of 0.6 nM for EGFR.
    • $74
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  • PP2
    T6266172889-27-9
    PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
    • $39
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  • Baricitinib phosphate
    T23601187595-84-1
    Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1 JAK2 inhibitor.
    • $40
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  • Vecabrutinib
    T172201510829-06-7
    Vecabrutinib (SNS-062) is a potent, noncovalent inhibitor of BTK (Kd: 0.3 nM) and ITK (Kd: 2.2 nM), with an IC50 of 24 nM for ITK.
    • $79
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  • ZAP-180013
    T8697873080-25-2
    ZAP-180013 is an inhibitor of zeta-chain-associated protein kinase 70 (ZAP70,IC50 : 1.8 μM).
    • $64
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  • Cerdulatinib
    T24871198300-79-6
    Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.
    • $37
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  • NVP-AEW541
    T6080475489-16-8
    NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.
    • $41
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  • HNMPA-(AM)3
    T36584120944-03-8
    HNMPA-(AM)3 inhibits activation of ERK phosphorylation and stimulation of ecdysteroid production by prothyrotropin (PTTH). Furthermore, HNMPA-(AM)3 had inhibitory effects on ecdysteroid production (IC50=14.2 μM) and insulin receptor activity (IC50=14.2 μM and 200 μM, in mosquitoes and mammals, respectively).
    • $197
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  • Ruxolitinib (S enantiomer)
    T6156941685-37-6
    Ruxolitinib S enantiomer (INCB18424) is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
    • $58
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  • AMG 900
    T6380945595-80-2
    AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A B C with IC50 values of 5 nM, 4 nM, and 1 nM, respectively. It exhibits over 10-fold selectivity for Aurora kinases compared to p38α, Tyk2, JNK2, Met, and Tie2. [Phase 1].
    • $44
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  • AZ7550
    T135641421373-99-0
    AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).
    • $133
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  • GSK 3 Inhibitor IX
    T1917667463-62-9
    GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.
    • $37
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  • Vidarabine
    T15065536-17-4
    Vidarabine (Adenine Arabinoside) is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.
    • $38
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  • Paltimatrectinib
    T624472353522-15-1
    Paltimatrectinib (PBI-200) is a potent tyrosine kinase inhibitor with anticancer activity that inhibits myosin-related kinase A (TrkA).Paltimatrectinib is used in the study of bladder, breast and colorectal cancers.
    • $199
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  • GLPG0634 analog
    T30761206101-20-3
    GLPG0634 analog (GLPG0634 analogue) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
    • $29
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  • Ilginatinib hydrochloride
    T12266L21239358-85-0
    Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.
    • $94
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  • GTP-14564
    T7185734823-86-4
    GTP-14564 is a novel tyrosine kinase inhibitor that also inhibits wt-FLT3 and ITD-FLT3. GTP-14564 inhibits the growth of interleukin-3-independent Ba/F1 expressing ITD-FLT3 at 3 μ m, whereas a 30-fold higher concentration of GTP-14564 is required to inhibit the FLT3 ligand-dependent growth (wt-FLT3) of Ba/F3 expressing wild-type FLT3. F3 expressing wild-type FLT3 (wt-FLT3).
    • $39
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  • SAR-20347
    T42101450881-55-6
    SAR-20347 is an inhibitor of TYK2 and JAK1 2 3, with IC50 values of 0.6 nM, 23 nM, 26 nM, and 41 nM, respectively.
    • $32
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  • NVP-BSK805 2HCl (1092499-93-8(free base))
    T6294 In house
    NVP-BSK805 2HCl (1092499-93-8(free base)) (BSK 805)(IC50=0.5 nM), a specific and effective ATP-competitive JAK2 inhibitor, is more than 20-fold specificity over JAK1, JAK3 and TYK2.
    • $53
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  • Brepocitinib
    TQ00101883299-62-4
    Brepocitinib (PF-06700841) is a potent dual JAK1 TYK2 inhibitor with IC50 values of 17 nM and 23 nM, respectively, and also inhibits JAK2 and JAK3 with IC50 values of 77 nM and 6.49 μM.
    • $30
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  • SU 5616
    T72021186611-58-5
    SU 5616 (WAY-608241) regulates abnormal cell proliferation and modulates tyrosine kinase signaling.
    • $48
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  • BMS-911543
    T67901271022-90-2
    BMS-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.
    • $31
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  • ST271
    T4511106392-48-7
    ST271 is an effective protein tyrosine kinase (PTK) inhibitor.
    • $33
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  • Tafetinib
    T289111032265-57-8In house
    Tafetinib (SIM-010603) is a novel potent and orally available tyrosine kinase inhibitor with anti-angiogenic and anti-tumour activity.
    • $250
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  • Tyrphostin AG30
    T7101122520-79-0
    Tyrphostin AG30 (AG30) (AG30) is a potent protein tyrosine kinases (PTK) inhibitor.
    • $39
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  • Syk Inhibitor II dihydrochloride
    T4391227449-73-2
    Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibit
    • $132
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  • NDI-034858
    T629022272904-53-5
    NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd<200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases caused by aberrant expression of IL12 and IL23.
    • $263
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  • EGFR-IN-87
    T798881835666-87-9In house
    EGFR-IN-87 is a potent EGFR tyrosine kinase inhibitor with anticancer activity that inhibits EGFR_d746-750, EGFR_L858R/T790M, and EGFR_WT in A431 cells, and can be used for cancer research.
    • $195
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  • SU 4981
    T60094186610-88-8
    SU 4981 is an inhibitor of VEGFR and a modulator of tyrosine kinase activity.
    • $117
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