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Proteases/Proteasome Tyrosine Kinases

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.
Cat No. product name
T1506 Vidarabine Vidarabine is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA...
T1835 IbrutinibHOT Ibrutinib is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
T1917 6-BIO BIO is a specific inhibitor of GSK-3.
T1929 Filgotinib GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
T1936 Alectinib CH5424802 is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.
T2360 Baricitinib Phosphate Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
T2382 VemurafenibHOT Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM).
T2473 PLX4720HOT PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).
T2485 Baricitinib Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activit...
T2636 Decernotinib Decernotinib(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.
T3061 Lorlatinib PF-06463922 is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), wi...
T3080 Pyridone 6 Pyridone 6(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 sign...
T4209 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...
T4210 SAR-20347 SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
T4511 ST 271 ST271 is an effective protein tyrosine kinase (PTK) inhibitor.
T6020 Pacritinib Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
T6080 NVP-AEW541 NVP-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.
T6104 Cerdulatinib hydrochloride 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 ...
T6156 S-Ruxolitinib Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
T6266 PP2 PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
T5049 NVP-BSK805 NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
T6343 Geldanamycin Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
T6380 AMG-900 AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases...
T6790 BMS-911543 BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
T6914 Oclacitinib maleate <p>Oclacitinib 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, w...
T4349 Sitravatinib Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
T7101 Tyrphostin AG30(AG30) Tyrphostin AG30 (AG30) is a potent protein tyrosine kinases (PTK) inhibitor.
TQ0010 PF-06700841 PF-06700841 is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). It also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
T2487 Cerdulatinib Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
T1829 (R)-RuxolitinibHOT Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
T1181 GefitinibHOT Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM).
T3076 GLPG0634 analogue GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
T4391 Syk Inhibitor II (hydrochloride) Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ cha...
T7945 SU14813 SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ...
T14669 BMS-066 BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
T14687 BMS-986165 BMS-986165 inhibits IL-12/23 and type I IFN pathways. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoi...
T15096 Delgocitinib Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
T13233 Tyk2-IN-3 Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase(IC50 of 485 nM).
Vidarabine
T1506CAS 5536-17-4
Vidarabine is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA...
Ibrutinib HOT
T1835CAS 936563-96-1
Ibrutinib is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
6-BIO
T1917CAS 667463-62-9
BIO is a specific inhibitor of GSK-3.
Filgotinib
T1929CAS 1206161-97-8
GLPG0634(filgotinib) is a selective JAK1 inhibitor. The IC50 values against JAK1, JAK2, JAK3, and TYK2 are 10 nM, 28 nM, 810 nM, and 116 nM, respectively.
Alectinib
T1936CAS 1256580-46-7
CH5424802 is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.
Baricitinib Phosphate
T2360CAS 1187595-84-1
Baricitinib phosphate is a selective orally bioavailable JAK1/JAK2 inhibitor.
Vemurafenib HOT
T2382CAS 918504-65-1
Vemurafenib (PLX4032) is a novel and potent B-Raf (V600E) inhibitor (IC50: 31 nM).
PLX4720 HOT
T2473CAS 918505-84-7
PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).
Baricitinib
T2485CAS 1187594-09-7
Baricitinib is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activit...
Decernotinib
T2636CAS 944842-54-0
Decernotinib(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.
Lorlatinib
T3061CAS 1454846-35-5
PF-06463922 is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), wi...
Pyridone 6
T3080CAS 457081-03-7
Pyridone 6(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 sign...
TAK-659 hydrochloride
T4209CAS 1952251-28-3
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...
SAR-20347
T4210CAS 1450881-55-6
SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).
ST 271
T4511CAS 106392-48-7
ST271 is an effective protein tyrosine kinase (PTK) inhibitor.
Pacritinib
T6020CAS 937272-79-2
Pacritinib (SB1518) is an effective and specific inhibitor of JAK2 and FLT3 (IC50: 23/22 nM, in cell-free assays).
NVP-AEW541
T6080CAS 475489-16-8
NVP-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.
Cerdulatinib hydrochloride
T6104CAS 1369761-01-2
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 ...
S-Ruxolitinib
T6156CAS 941685-37-6
Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib is the first potent, selective JAK1/2 inhibitor.
PP2
T6266CAS 172889-27-9
PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
NVP-BSK805
T5049CAS 1092499-93-8
NVP-BSK805 is an ATP-competitive JAK2 inhibitor.
Geldanamycin
T6343CAS 30562-34-6
Geldanamycin, an HSP90 inhibitor (Kd: 1.2 μM), specifically disrupts glucocorticoid receptor (GR)/HSP association.
AMG-900
T6380CAS 945595-80-2
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM. It is >10-fold selective for Aurora kinases...
BMS-911543
T6790CAS 1271022-90-2
BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1nM, ~350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively. Phase 1/2.
Oclacitinib maleate
T6914CAS 1640292-55-2
<p>Oclacitinib 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, w...
Sitravatinib
T4349CAS 1123837-84-2
Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.
Tyrphostin AG30(AG30)
T7101CAS 122520-79-0
Tyrphostin AG30 (AG30) is a potent protein tyrosine kinases (PTK) inhibitor.
PF-06700841
TQ0010CAS 1883299-62-4
PF-06700841 is a potent dual JAK1/TYK2 inhibitor (IC50s: 17 nM/23 nM). It also inhibits JAK2/3 (IC50s: 77 nM/6.49 μM).
Cerdulatinib
T2487CAS 1198300-79-6
Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
(R)-Ruxolitinib HOT
T1829CAS 941678-49-5
Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC50: 3.3/2.8 nM) and is relatively less selective for JAK3 (IC50: 322 nM).
Gefitinib HOT
T1181CAS 184475-35-2
Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM).
GLPG0634 analogue
T3076CAS 1206101-20-3
GLPG0634 (analog) is a specific JAK1 inhibitor with IC50 of 10/28/810/116 nM for JAK1/2/3 and TYK2, respectively.
Syk Inhibitor II (hydrochloride)
T4391CAS 227449-73-2
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ cha...
SU14813
T7945CAS 627908-92-3
SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ...
BMS-066
T14669CAS 914946-88-6
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor. With IC50s of 9 nM and 72 nM, respectively.
BMS-986165
T14687CAS 1609392-27-9
BMS-986165 inhibits IL-12/23 and type I IFN pathways. BMS-986165 is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoi...
Delgocitinib
T15096CAS 1263774-59-9
Delgocitinib is a novel and specific inhibitor of JAK (IC50s: 2.8, 2.6, 13, and 58 nM for JAK1, JAK2, JAK3, and Tyk2).
Tyk2-IN-3
T13233CAS 1779493-12-7
Tyk2-IN-3 is an inhibitor of Tyk2 pseudokinase(IC50 of 485 nM).