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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

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.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsTyrosine Kinases

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.

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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.

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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.

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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.

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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.

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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.

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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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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).

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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.

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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.

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Peficitinib

T6933944118-01-8

Peficitinib (ASP015K) (ASP015K, JNJ-54781532) is an orally bioavailable JAK inhibitor. Phase 3.

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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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Geldanamycin

T634330562-34-6

Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR) HSP association.

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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.

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Ilginatinib

T122661239358-86-1

Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor.

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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.

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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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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.

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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.

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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.

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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].

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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.

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Baricitinib phosphate

T23601187595-84-1

Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1 JAK2 inhibitor.

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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).

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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.

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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.

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Cerdulatinib

T24871198300-79-6

Cerdulatinib (PRT2070) is an novel oral dual Syk JAK inhibitor.

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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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Ilginatinib hydrochloride

T12266L21239358-85-0

Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.

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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.

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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.

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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.

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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).

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Merestinib dihydrochloride

T158081206801-37-7

Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally available kinase inhibitor with antitumor activity that inhibits MET, AXL, RON, and MKNK1 2, and inhibits the growth of NTRK fusion-carrying tumors.

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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.

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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.

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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.

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SU 5616

T72021186611-58-5

SU 5616 (WAY-608241) regulates abnormal cell proliferation and modulates tyrosine kinase signaling.

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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.

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ST271

T4511106392-48-7

ST271 is an effective protein tyrosine kinase (PTK) inhibitor.

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Tyrphostin AG30

T7101122520-79-0

Tyrphostin AG30 (AG30) (AG30) is a potent protein tyrosine kinases (PTK) inhibitor.

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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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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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Vamotinib

T637461416241-23-0In house

Vamotinib (PF-114) is an orally active and specific tyrosine kinase inhibitor with antiproliferative and antitumour activity.Vamotinib inhibits the phosphorylation of BCR ABL and BCR ABL-T315I, which promotes apoptosis. Vamotinib is used to study drug-resistant Philadelphia chromosome-positive (Ph+) leukaemia and Alzheimer's disease.

$108

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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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