Search Result
Results for "
Tyrosine Inhibitors
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
73
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-148810
-
|
BI 1810631
|
c-Met/HGFR
|
Cancer
|
|
Zongertinib (BI 1810631) is a potent and selective HER2 and EGFR tyrosine kinase inhibitor with IC50 values of 13 nM and 579 nM, respectively. Zongertinib has antitumor activity and can be used in the study of multiple solid tumors .
|
-
-
- HY-10158
-
|
SKI-606
|
Src
Bcr-Abl
Autophagy
|
Cancer
|
|
Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively .
|
-
-
- HY-127178
-
|
|
Phosphatase
|
Cancer
|
|
ML120 analog 1 (compound 1) is a competitive inhibitor with a Ki of 0.69 μM for Hematopoietic protein tyrosine phosphatase (HePTP) .
|
-
-
- HY-162489
-
|
|
Bcr-Abl
|
Others
|
|
Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia .
|
-
-
- HY-110367
-
|
|
Src
|
Others
|
|
LCB 03-0110 dihydrochloride is a dihydrochloride of LCB 03-0110. LCB 03-0110 is a potent inhibitor of Src family tyrosine kinase .
|
-
-
- HY-148832
-
|
|
Btk
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-20 (compound 283) is a BTK tyrosine kinase inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. BTK-IN-20 can be used for the research of cancer and inflammation .
|
-
-
- HY-N12177
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively .
|
-
-
- HY-10158R
-
|
|
Src
Bcr-Abl
Autophagy
|
Cancer
|
|
Bosutinib (Standard) is the analytical standard of Bosutinib. This product is intended for research and analytical applications. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively .
|
-
-
- HY-142680
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .
|
-
-
- HY-124146
-
|
|
Syk
|
Inflammation/Immunology
|
|
BI1002494 is an orally active, potent, and selective spleen tyrosine kinase (SYK) inhibitor. BI 1002494 exhibits an IC50 of 115 nM in inhibiting high-affinity IgE receptor-mediated mast cell and basophil degranulation. BI1002494 can be utilized in immunology reesearch .
|
-
-
- HY-146680
-
|
|
FLT3
RET
CDK
MAP4K
|
Cancer
|
|
FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research .
|
-
-
- HY-156092
-
|
|
BCRP
Apoptosis
|
Cancer
|
|
Antitumor photosensitizer-4 (compound 10b) is a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. Antitumor photosensitizer-4 is a photosensitizer (PS) consisting of a conjugate of dasatinib (HY-10181) and imatinib (HY-15463). Antitumor photosensitizer-4 induces apoptosis and ROS production and exhibits strong phototoxicity to HepG2 and B16-F10 cells .
|
-
-
- HY-N10378
-
|
|
Phosphatase
|
Neurological Disease
Metabolic Disease
|
|
Rubrofusarin 6-O-β-D-glucopyranoside, the glycoside of Rubrofusarin, is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with the IC50 of 87.36 μM. Rubrofusarin 6-O-β-D-glucopyranoside can be used for the research of comorbid diabetes and depression .
|
-
-
- HY-10421
-
|
|
c-Met/HGFR
|
Cancer
|
|
Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor.
|
-
-
- HY-112823A
-
|
HS-10296 mesylate
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
|
-
-
- HY-Y0444S
-
|
|
Isotope-Labeled Compounds
Tyrosinase
|
Metabolic Disease
|
|
D-Tyrosine-d2 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
|
-
-
- HY-Y0444S1
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
D-Tyrosine-d4 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
|
-
-
- HY-Y0444S2
-
|
|
Isotope-Labeled Compounds
Tyrosinase
|
Metabolic Disease
|
|
D-Tyrosine-d7 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
|
-
-
- HY-33549
-
|
|
Others
|
Neurological Disease
Cancer
|
|
α-Methyl-p-tyrosine is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. α-Methyl-p-tyrosine can be used in research related to epilepsy, glaucoma, cancer, and other related diseases .
|
-
-
- HY-Y0444
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth .
|
-
-
- HY-W104477
-
|
|
Others
|
Metabolic Disease
|
|
3-Fluoro-L-tyrosine is a tyrosine analogue, inhibits transamination by tyrosine aminotransferase (TAT). And 3-FluoroL-tyrosine has been shown to be biologically incorporated into proteins in place of tyrosine. 3-Fluoro-L-tyrosine pretends to be the substrate of rat liver tyrosine aminotransferase, markedly disturbs the Tyr-TAT association .
|
-
-
- HY-112412
-
|
PDGF Receptor Tyrosine Kinase Inhibitor III
|
PDGFR
|
Neurological Disease
|
|
PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III), a multikinase inhibitor, inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis .
|
-
-
- HY-147612
-
|
|
c-Met/HGFR
|
Cancer
|
|
Tyrosine kinase-IN-4 (EXAMPLE 107) is a protein tyrosine kinase inhibitor .
|
-
-
- HY-121889
-
|
|
Tyrosinase
|
Inflammation/Immunology
|
|
FQ is a tyrosinase inhibitor that effectively inhibits the diphenolase activity of mushroom tyrosinase (IC50=120 μM). FQ can be used in the study of pigmentation .
|
-
-
- HY-N0473S8
-
-
-
- HY-N0473S9
-
-
-
- HY-N0473S14
-
-
-
- HY-N0473S15
-
-
-
- HY-N0473S1
-
-
-
- HY-N0473S12
-
-
-
- HY-N0473S4
-
-
-
- HY-N0473S13
-
-
-
- HY-50946
-
|
STI571 Mesylate; CGP-57148B Mesylate
|
c-Kit
Bcr-Abl
PDGFR
Autophagy
|
Cancer
|
|
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
|
-
-
- HY-N0473S
-
-
-
- HY-N0473S2
-
-
-
- HY-N0473S3
-
-
-
- HY-N0473S5
-
-
-
- HY-N0473S7
-
-
-
- HY-N0473R
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
L-Tyrosine (Standard) is the analytical standard of L-Tyrosine. This product is intended for research and analytical applications. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
|
-
-
- HY-N0473S6
-
-
-
- HY-N0473S11
-
-
-
- HY-N0473S16
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
L-Tyrosine- 13C, 15N is the 13C and 15N labeled L-Tyrosine[1]. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex[2].
|
-
-
- HY-156619
-
|
|
c-Kit
|
Cancer
|
|
Labuxtinib is c-kit tyrosine kinase inhibitor .
|
-
-
- HY-50946R
-
|
STI571 Mesylate (Standard); CGP-57148B Mesylate (Standard)
|
c-Kit
Bcr-Abl
PDGFR
Autophagy
|
Cancer
|
|
Imatinib (Mesylate) (Standard) is the analytical standard of Imatinib (Mesylate). This product is intended for research and analytical applications. Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
|
-
-
- HY-131005
-
-
-
- HY-111158
-
|
|
c-Met/HGFR
|
Cancer
|
|
BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML) .
|
-
-
- HY-152852A
-
|
Mifanertinib dimaleate
|
c-Met/HGFR
|
Cancer
|
|
Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
|
-
-
- HY-156640
-
|
LP-168
|
Others
|
Cancer
|
|
Rocbrutinib is a Bruton's tyrosine kinase inhibitor with antineoplastic effect .
|
-
-
- HY-101962
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities
|
-
-
- HY-125260
-
|
|
SHP2
|
Cancer
|
|
SHP844 is a SHP2 inhibitor with the IC50 of 18.9 µM. SHP2 is a protein tyrosine phosphatase (PTP) that regulates tyrosine phosphorylation levels and is involved in cell proliferation, differentiation and survival .
|
-
- HY-50686
-
|
ARQ 197; (3R,4R)-ARQ 198
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
Tivantinib is a highly selective c-Met tyrosine kinase inhibitor with a Ki of 355 nM.
|
-
- HY-112446
-
-
- HY-152830
-
|
|
c-Met/HGFR
|
Cancer
|
|
Adrixetinib is an inhibitor of protein tyrosine kinase with antineoplastic activity .
|
-
- HY-152840
-
|
|
c-Met/HGFR
|
Cancer
|
|
Emzeltrectinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
|
-
- HY-18016
-
-
- HY-W013478
-
|
|
Phosphatase
|
Cancer
|
|
PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect .
|
-
- HY-114667
-
|
|
EGFR
|
Others
|
|
Lavendustin C6 is a specific inhibitor of tyrosine kinase. Lavendustin C6 inhibits epidermal growth factor (EGF) receptor tyrosine kinase with an EC50 value of 0.05 μg/mL. Lavendustin C6 inhibits platelet-derived growth factor (PDGF)-induced inositol phosphate formation .
|
-
- HY-101756
-
|
SDZ-LAP 977
|
EGFR
|
Cancer
|
|
SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
|
-
- HY-10159
-
|
AMN107
|
Bcr-Abl
Autophagy
|
Cancer
|
|
Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
|
-
- HY-107594
-
|
|
JAK
|
Cancer
|
|
Benzene hexabromide, a bromohydrocarbon, is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation.
|
-
- HY-152852
-
|
Mifanertinib
|
c-Met/HGFR
|
Cancer
|
|
Mefatinib free base is a potent tyrosine kinase inhibitor with antineoplastic activity .
|
-
- HY-159840
-
|
|
FGFR
|
Cancer
|
|
Fanregratinib is a fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitor .
|
-
- HY-101429
-
RG13022
1 Publications Verification
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-112139
-
|
|
Phosphatase
|
Others
|
|
4-(Bromoacetyl)phenoxyacetic acid (PTP inhibitor III) is a protein tyrosine phosphatase (PTP) inhibitor .
|
-
- HY-18840
-
BBT594
3 Publications Verification
NVP-BBT594
|
RET
|
Cancer
|
|
BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
|
-
- HY-101296
-
|
|
FGFR
Autophagy
|
Cancer
|
|
PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
|
-
- HY-149895
-
|
|
Syk
|
Cancer
|
|
Syk-IN-7 (compound 17) is an inhibitor of spleen tyrosine kinase (SYK) .
|
-
- HY-111781
-
|
WS-413
|
Others
|
Cancer
|
|
Civorebrutinib (WS-413) is a Bruton's tyrosine kinase inhibitor with antineoplastic effect .
|
-
- HY-156632
-
|
KIN-3248
|
FGFR
|
Cancer
|
|
Resigratinib (KIN-3248) is a FGFR tyrosine kinase inhibitor, with antineoplastic effect .
|
-
- HY-152830A
-
|
|
Others
|
Cancer
|
|
Adrixetinib (TFA) is an inhibitor of protein tyrosine kinase with antineoplastic activity .
|
-
- HY-159503
-
|
3D185 free base; HH185 free base
|
Others
|
Cancer
|
|
Segigratinib is a fibroblast growth factor receptor tyrosine kinase inhibitor, with antineoplastic effect .
|
-
- HY-135564B
-
|
|
Phosphatase
|
Cancer
|
|
(Rac)-RK-682, a racemate of RK-682, is a protein tyrosine phosphatases (PTPases) inhibitor. (Rac)-RK-682 inhibits protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B) with IC50s of 8.6 μM, 12.4 μM, and 0.7 μM, respectively .
|
-
- HY-101246
-
|
|
RET
|
Cancer
|
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
|
-
- HY-117718
-
|
Tyrphostin AG957; NSC 654705
|
Bcr-Abl
|
Cancer
|
|
AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity . AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210 bcr/abl autokinase activity .
|
-
- HY-12312
-
-
- HY-100335
-
|
|
Btk
|
Others
|
|
PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
|
-
- HY-164718
-
|
|
EGFR
|
Cancer
|
|
Sevabertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor activity .
|
-
- HY-10331S
-
|
BAY 73-4506-d3
|
VEGFR
Autophagy
PDGFR
Raf
RET
|
Cancer
|
|
Regorafenib-d3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor[1].
|
-
- HY-130255
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM .
|
-
- HY-101474S
-
|
BGB-3111 d5
|
Btk
|
Cancer
|
|
Zanubrutinib-d5 is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor[1].
|
-
- HY-15333
-
-
- HY-D0852
-
|
|
Phosphatase
|
Cancer
|
|
Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
|
-
- HY-12974
-
|
PRT318
|
Syk
|
Cancer
|
|
PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM.
|
-
- HY-N0473
-
-
- HY-108484
-
|
|
EGFR
|
Cancer
|
|
PP 3 (Compound 3) is an EGFR tyrosine kinase inhibitor with an IC50 of 2.7 μM .
|
-
- HY-153941
-
|
|
RET
|
Cancer
|
|
RET-IN-24 (Compound 26) is a selective RET tyrosine kinase inhibitor with antitumor activity .
|
-
- HY-12000
-
|
Tyrphostin AG490; Tyrphostin B42
|
EGFR
STAT
JAK
Autophagy
|
Cancer
|
|
AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
|
-
- HY-111489B
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-N5118
-
|
(-)-Chimonanthine
|
Tyrosinase
|
Cancer
|
|
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis .
|
-
- HY-111489A
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP inhibitor 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-111489
-
|
|
Phosphatase
|
Metabolic Disease
|
|
LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
|
-
- HY-161695
-
|
|
Others
|
Cancer
|
|
Angiogenesis inhibitor 6 (Compound 8) is a non-tyrosine kinase inhibitor with effective antiangiogenic properties. Angiogenesis inhibitor 6 has antitumor activity .
|
-
- HY-N0198
-
-
- HY-12963
-
|
TP-0903
|
TAM Receptor
Apoptosis
|
Cancer
|
|
Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
|
-
- HY-18007
-
|
Eph receptor Tyrosine kinase inhibitor
|
Ephrin Receptor
|
Cancer
|
|
ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
|
-
- HY-101793
-
|
|
Btk
|
Inflammation/Immunology
|
|
BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
|
-
- HY-18316
-
-
- HY-117253
-
|
|
Drug Metabolite
|
Cancer
|
|
PHA-782584 is a metabolite of sunitinib. Sunitinib is an oral multitargeted tyrosine kinase inhibitor with antitumor activities .
|
-
- HY-162355
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-27 (compound 28) is an allosteric inhibitor of tyrosine phosphatase SH2 .
|
-
- HY-12312A
-
-
- HY-100463
-
-
- HY-10338
-
|
XL880; GSK1363089; GSK089; EXEL-2880
|
VEGFR
c-Met/HGFR
|
Cancer
|
|
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
|
-
- HY-13804
-
|
AGL 1872; EI 275
|
Src
Apoptosis
|
Cancer
|
|
PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC50 of 5 and 6 nM for Lck and Fyn, respectively.
|
-
- HY-101856
-
|
|
Btk
|
Inflammation/Immunology
|
|
BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
|
-
- HY-101820
-
|
|
EGFR
|
Cancer
|
|
Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-117155
-
PKI-166
1 Publications Verification
|
EGFR
|
Cancer
|
|
PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM .
|
-
- HY-110328
-
|
|
EGFR
|
Cancer
|
|
PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM .
|
-
- HY-101820A
-
|
|
EGFR
|
Cancer
|
|
Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities .
|
-
- HY-109082A
-
|
SKI-O-703 dimesylate
|
Syk
|
Inflammation/Immunology
|
|
Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities .
|
-
- HY-20878
-
|
AG 879
|
Trk Receptor
EGFR
Apoptosis
|
Cancer
|
|
Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity .
|
-
- HY-101053
-
|
Src Kinase Inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-101766
-
|
BGB-3111 analog
|
Btk
|
Inflammation/Immunology
|
|
Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
|
-
- HY-15656S
-
-
- HY-101959A
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Tyrphostin 47 is a nonspecific inhibitor of WNK1. Tyrphostin 47 is a protein tyrosine kinase inhibitor. Tyrphostin 47 inhibits smooth-muscle cell proliferation
|
-
- HY-149636
-
|
|
EGFR
CDK
VEGFR
|
Cancer
|
|
Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
|
-
- HY-156912
-
|
|
EGFR
|
Cancer
|
|
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .
|
-
- HY-101474B
-
|
(R)-BGB-3111
|
Btk
|
Others
|
|
(R)-Zanubrutinib is the R enantiomer of Zanubrutinib (HY-101474A). (R)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 11 nM.
|
-
- HY-10181S
-
-
- HY-128576
-
|
|
Others
|
Cancer
|
|
DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity .
|
-
- HY-115496
-
-
- HY-N2506
-
|
|
Others
|
Cardiovascular Disease
|
|
Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation .
|
-
- HY-133083
-
|
|
c-Met/HGFR
|
Cancer
|
|
BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe .
|
-
- HY-155812
-
|
|
c-Met/HGFR
|
Cancer
|
|
Tyrosine kinase-IN-6 is a potent and promising RON splice variants inhibitor with anti-cancer and o?antineoplastic effects .
|
-
- HY-125350
-
|
Tyrphostin AG1290
|
c-Met/HGFR
|
Metabolic Disease
|
|
Entacapone acid (Tyrphostin AG1290) is a tyrosine kinase inhibitor. Entacapone acid reduces hepatic protein synthesis rate (HPS) in vivo .
|
-
- HY-148742
-
|
|
RET
|
Cancer
|
|
RET-IN-21 is an inhibitor of receptor tyrosine kinase (RET), with the IC 50 of 4.4 μM, that has antitumor activity .
|
-
- HY-161731
-
|
|
Others
|
Cancer
|
|
DS08701581 is an inhibitor of FER tyrosine kinase with IC50. DS08701581 has anti-tumor activity and oral activity .
|
-
- HY-19779
-
|
|
Phosphatase
|
Metabolic Disease
|
|
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
|
-
- HY-50878
-
|
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-50878B
-
|
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-101474A
-
|
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC50: 0.3 nM) .
|
-
- HY-112096
-
eCF506
2 Publications Verification
|
Src
|
Cancer
|
|
eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.
|
-
- HY-112166
-
|
PRN1008
|
Btk
|
Metabolic Disease
Cancer
|
|
Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
|
-
- HY-152845
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Ficonalkib is a potent inhibitor of Anaplastic lymphoma kinase (ALK), the tyrosine kinase receptor. Ficonalkib, can be used as an antineoplastic agent .
|
-
- HY-153110A
-
|
|
EGFR
IRAK
Btk
|
Cancer
|
|
Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM .
|
-
- HY-153110
-
|
|
EGFR
IRAK
Btk
|
Cancer
|
|
Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM .
|
-
- HY-156603
-
|
|
c-Met/HGFR
|
Cancer
|
|
Canlitinib is a tyrosine kinase inhibitor, extracted from patent WO2018072614 (IV-2). Canlitinib has the potential for cancer study.
|
-
- HY-13892
-
|
CHIR-258 dilactic acid; TKI258 dilactic acid
|
VEGFR
|
Cancer
|
|
Dovitinib (dilactic acid) is an orally active inhibitor of VEGF kinase. Dovitinib (dilactic acid) inhibits receptor tyrosine kinases (RTKs) involved in solid and hematologic cancers and tumor angiogenesis .
|
-
- HY-162156
-
|
|
Others
|
Cancer
|
|
TTK inhibitor 4 (compound 16) is a potent inhibitor of threonine tyrosine kinase (TTK), with the IC50 value of 0.016 μM, that has anti-tumor activity .
|
-
- HY-101961
-
|
AG 1288
|
c-Kit
|
Inflammation/Immunology
|
|
Tyrphostin AG 1288 is a potent Tyrosine Kinase inhibitor. Tyrphostin AG 1288 inhibits ICAM1 expression and TNFα-mediated cytotoxicity in vitro .
|
-
- HY-164413
-
|
|
VEGFR
EGFR
RET
Apoptosis
|
Cancer
|
|
CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways .
|
-
- HY-132808
-
|
SAR 444727; PRN473
|
Btk
|
Inflammation/Immunology
|
|
Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .
|
-
- HY-10644
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck inhibitor 2 is a multi-target tyrosine kinase inhibitor with IC50s of 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively.
|
-
- HY-101474
-
|
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC50 of 0.63 nM .
|
-
- HY-147303
-
|
|
Trk Receptor
EGFR
|
Cancer
|
|
Sacibertinib is a tyrosine kinase (Trk) inhibitor with EC50 value of 110 nM and 244 nM for EGFR-TK phosphorylation and HER2, respectively. Antineoplastic activity .
|
-
- HY-152839A
-
|
BLU-263 phosphate
|
c-Kit
|
Cancer
|
|
Elenestinib phosphate (BLU-263 phosphate) is a potent and orally active tyrosine kinase inhibitor. Elenestinib phosphate has the potential for the research of systemic mastocytosis (SM) .
|
-
- HY-156604
-
|
|
Btk
|
Cancer
|
|
Cinsebrutinib is a Bruton's tyrosine kinase inhibitor, extracted from patent WO2021207549 (compound 5-6). Cinsebrutinib has the potential for cancer study.
|
-
- HY-124152
-
|
Methyl-3,4-dephostatin
|
MAP3K
MAP4K
Phosphatase
|
Neurological Disease
|
|
3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase .
|
-
- HY-50878S
-
|
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-10159A
-
|
AMN107 monohydrochloride monohydrate
|
Bcr-Abl
Autophagy
|
Cancer
|
|
Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
|
-
- HY-100462
-
-
- HY-100314
-
|
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
|
-
- HY-10159S
-
|
AMN107-d6
|
Bcr-Abl
Autophagy
|
Cancer
|
|
Nilotinib-d6 is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity[1].
|
-
- HY-138202
-
|
|
Src
|
Inflammation/Immunology
|
|
Lck-IN-1 is a potent lymphocyte protein tyrosine kinase (Lck) inhibitor extracted from patent WO2007013673A1, example 48 .
|
-
- HY-112405
-
|
PD 159121
|
EGFR
|
Cancer
|
|
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively .
|
-
- HY-156625
-
|
NFX-179
|
MEK
|
Cancer
|
|
Nedometinib is a tyrosine kinase inhibitor targeting to MEK1. Nedometinib has antineoplastic effect and can be used for research in dermatosis, cutaneous fibroneuroma, neurofibromatosis .
|
-
- HY-W062695
-
|
(R)-ACP-196
|
Btk
|
Cancer
|
|
(R)-Acalabrutinib ((R)-ACP-196) is the enantiomer of Acalabrutinib (HY-17600). (R)-Acalabrutinib is an inhibitor for Bruton’s tyrosine kinase (BTK) .
|
-
- HY-138317
-
|
|
Others
|
Cancer
|
|
Tyk2-IN-10 (compound 17.5) is a tyrosine kinase 2-mediated signaling inhibitor involved in inflammation regulation .
|
-
- HY-142517
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .
|
-
- HY-142519
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511) .
|
-
- HY-10158A
-
|
SKI-606 hydrate
|
Src
Bcr-Abl
|
Cancer
|
|
Bosutinib (hydrate) is an oral Src/Abl tyrosine kinase inhibito with IC50 of 1.2 nM and 1 nM, respectively .
|
-
- HY-N10649
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-21 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM), which is a key target for type 2 diabetes inhibition .
|
-
- HY-100625
-
-
- HY-155587
-
|
|
Others
|
Cancer
|
|
Hydroxy-PP is a potent CBR1 inhibitor with an IC50 value of 0.78 μM. Hydroxy-PP also potently inhibits the cytoplasmic tyrosine kinase Fyn with an IC50 value of 5 nM .
|
-
- HY-135725
-
|
|
EGFR
|
Cancer
|
|
D-69491 hydrochloride is a HER-2 tyrosine kinase inhibitor that reduces HER-2 phosphorylation, inhibits the proliferation of SKOV-3 cells, and has anticancer activity .
|
-
- HY-10407
-
|
|
VEGFR
FGFR
PDGFR
|
Cancer
|
|
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
|
-
- HY-13455
-
|
|
Haspin Kinase
DYRK
|
Cancer
|
|
LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively .
|
-
- HY-132549S
-
-
- HY-13455A
-
|
|
Haspin Kinase
DYRK
|
Cancer
|
|
LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively .
|
-
- HY-101474BS
-
|
|
Btk
Isotope-Labeled Compounds
|
Others
|
|
(R)-Zanubrutinib-d5 is deuterium labeled (R)-Zanubrutinib. (R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
|
-
- HY-P99969
-
|
|
EGFR
|
Cancer
|
|
Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab alone or together with tyrosine kinase inhibitors has antitumor activities .
|
-
- HY-76688
-
|
(Rac)-ARQ 197; (Rac)-ARQ 198
|
Others
|
Cancer
|
|
(Rac)-Tivantinib is the isomer of Tivantinib (HY-50686), and can be used as an experimental control. Tivantinib is a highly selective c-Met tyrosine kinase inhibitor with a Ki of 355 nM.
|
-
- HY-156409
-
|
|
JAK
|
Inflammation/Immunology
|
|
ABBV-712 is a selective inhibitor of Tyrosine kinase 2 (TYK2), with IC50 of 0.195 μM, that play important role in autoimmune diseases .
|
-
- HY-10159R
-
|
|
Bcr-Abl
Autophagy
|
Cancer
|
|
Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
|
-
- HY-15492A
-
|
AG-013958 monohydrochloride
|
VEGFR
|
Cardiovascular Disease
|
|
AG-13958 monohydrochloride, a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD) .
|
-
- HY-19730A
-
|
HM61713 hydrochloride; BI 1482694 hydrochloride
|
EGFR
|
Cancer
|
|
Olmutinib hydrochloride is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib hydrochloride is used for NSCLC .
|
-
- HY-101959
-
|
AG213
|
EGFR
Topoisomerase
|
Cancer
|
|
Tyrphostin AG213 (AG213) is an inhibitor of epidermal growth factor receptor (EGFR) protein tyrosine kinase (IC50=0.85 μM). Tyrphostin AG213 inhibits tyrosine kinase activity IC50=2.4 μM) and topoisomerase II (IC100=50 μM). Tyrphostin AG213 can induce nonapoptotic cell programmed death in tumor cells .
|
-
- HY-12135
-
|
|
Polo-like Kinase (PLK)
PIN1
STAT
|
Cancer
|
Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC50 values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research .
|
-
- HY-10260
-
|
ZD6474
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
|
-
- HY-10260B
-
|
ZD6474 hydrochloride
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
|
-
- HY-10260A
-
|
ZD6474 trifluoroacetate
|
VEGFR
Autophagy
Apoptosis
|
Cancer
|
|
Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) .
|
-
- HY-N10648
-
|
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-20 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.05 μM) over the highly homologous T-cell protein tyrosine phosphatase (TCPTP; IC50=78.0 μM), which is a key target for type 2 diabetes inhibition .
|
-
- HY-13802
-
SC-514
5 Publications Verification
GK 01140
|
IKK
|
Cancer
|
|
SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
|
-
- HY-103097
-
|
|
Phospholipase
|
Others
|
|
ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
|
-
- HY-N1750
-
|
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively .
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-118304B
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
|
-
- HY-50878R
-
|
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-18667
-
|
|
Phosphatase
|
Inflammation/Immunology
|
|
LTV-1 is a potent lymphoid tyrosine phosphatase (LYP) inhibitor in T cells with an IC50 of 508 nM. LTV-1 has the potential for autoimmunity treatment .
|
-
- HY-100636
-
|
|
EGFR
|
Cancer
|
|
Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells .
|
-
- HY-12806
-
|
|
EGFR
|
Cancer
|
|
AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194 .
|
-
- HY-43521
-
|
|
Btk
|
Cancer
|
|
Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies .
|
-
- HY-145587
-
|
PBI-200; PPI-5278
|
Tyrosinase
Trk Receptor
|
Inflammation/Immunology
Cancer
|
|
Paltimatrectinib (compound I-147) is a potent tyrosine kinase inhibitor with an IC50 of <10 nM for tropomyosin kinases A (TrkA). Paltimatrectinib has the potential for cancer and inflammatory diseases .
|
-
- HY-10159B
-
|
AMN107 hydrochloride
|
Bcr-Abl
Autophagy
|
Cancer
|
Nilotinib (AMN107) hydrochloride is an orally active Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity and can be used in studies of chronic myelogenous leukaemia .
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-
- HY-N3267
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Methyl pseudolarate B, a natural diterpenoid, is a protein tyrosine phosphatase 1B (PTP1B) (Phosphatase) inhibitor with an IC50 value of 10.9 μM .
|
-
- HY-148811
-
|
ICP-723
|
c-Met/HGFR
|
Cancer
|
|
Zurletrectinib is a potent tyrosine kinase inhibitor. Zurletrectinib serves as an antineoplastic agent. Zurletrectinib can used for research of preventing TRK-mediated related diseases, such as tumors .
|
-
- HY-152849
-
|
HL5101
|
c-Met/HGFR
|
Cancer
|
|
Boditrectinib is a potent tyrosine kinase inhibitor. Boditrectinib serves as an antineoplastic agent. Boditrectinib is useful in the research of cancer, inflammation, neurodegenerative diseases and certain infectious diseases .
|
-
- HY-100636A
-
|
|
EGFR
|
Cancer
|
|
Gefitinib N-oxide hydrochloride is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells .
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-
- HY-152852S
-
|
Mifanertinib-d6
|
Isotope-Labeled Compounds
c-Met/HGFR
|
Cancer
|
|
Mefatinib-d6 free base (Mifanertinib-d6) is the deuterium labeled Mefatinib. Mefatinib is a potent tyrosine kinase inhibitor with antineoplastic activity .
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-
- HY-159820
-
|
|
Others
|
Cancer
|
|
Veonetinib (example 3) is a potent inhibitor of tyrosine kinase, with the IC50 of 0.1 μM and 0.4 μM in A549 cells and LOVO cells, respectively .
|
-
- HY-129510
-
|
|
EGFR
|
Cancer
|
|
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
|
-
- HY-14596
-
|
NPI 031L
|
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
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-
- HY-123390
-
|
|
Bcr-Abl
Akt
|
Cancer
|
|
DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM .
|
-
- HY-10322
-
|
BIBX 1382
|
EGFR
|
Cancer
|
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity .
|
-
- HY-120857
-
|
PD 158294
|
Others
|
Others
|
|
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50=8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR.
|
-
- HY-10501
-
SU14813
1 Publications Verification
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
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-
- HY-10501A
-
|
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
|
-
- HY-130680
-
|
|
Syk
|
Cancer
|
|
Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM .
|
-
- HY-50896S1
-
|
CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6
|
Isotope-Labeled Compounds
EGFR
Autophagy
|
Cancer
|
|
Erlotinib- 13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1].
|
-
- HY-15492
-
|
AG-013958
|
VEGFR
|
Cardiovascular Disease
|
|
AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD) .
|
-
- HY-50895S
-
|
ZD1839-d8
|
EGFR
Autophagy
|
Cancer
|
|
Gefitinib-d8 is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells[1][2].
|
-
- HY-100024
-
|
|
Others
|
Cancer
|
|
NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer .
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-
- HY-147316
-
|
|
Others
|
Cancer
|
|
TP-5801 is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity .
|
-
- HY-15728
-
|
IY-5511
|
Bcr-Abl
|
Cancer
|
|
Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.
|
-
- HY-161057
-
-
- HY-160167
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-30 (compound cpd15) is an inhibitor of Bruton's Tyrosine Kinase (BTK) and mutant BTK with IC50 values of 6.72 and 6.11nM respectively .
|
-
- HY-10159S1
-
-
- HY-118964
-
|
|
Others
|
Others
|
|
Tyrphostin AG 568 is a tyrphostin tyrosine kinase inhibitor that induces erythroid differentiation. Tyrphostin AG 568 can be utilized in research related to autologous bone marrow transplantation .
|
-
- HY-10981
-
|
E7080
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
|
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-108330
-
AG126
2 Publications Verification
Tyrphostin AG126
|
ERK
|
Inflammation/Immunology
|
|
AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research .
|
-
- HY-10981A
-
|
E7080 mesylate
|
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
|
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-123506
-
|
|
Src
|
Neurological Disease
Inflammation/Immunology
|
|
Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models .
|
-
- HY-110367A
-
|
|
Src
|
Others
|
|
LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor. LCB 03-0110 suppresses scar formation by inhibiting fibroblast and macrophage activation .
|
-
- HY-118304
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6?nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1?μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .
|
-
- HY-124827
-
|
|
Tyrosinase
|
Cancer
|
|
Tec-IN-1 (Compound 21) is a Tec inhibitor (IC50s of 11.7 μM). Tec-IN-1 inhibits Tec-mediated tyrosine phosphorylation of FGF2, and inhibits FGF2 secretion from cells .
|
-
- HY-112345
-
|
|
FGFR
PDGFR
EGFR
Src
|
Cancer
|
|
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .
|
-
- HY-80002
-
|
BMX kinase inhibitor
|
Btk
BMX Kinase
|
Cancer
|
|
BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
|
-
- HY-100867A
-
|
TAK-659 monohydrochloride; CB-659 monohydrochloride
|
Syk
FLT3
|
Cancer
|
|
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-100867
-
|
TAK-659; CB-659
|
Syk
FLT3
|
Cancer
|
|
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-N4185
-
|
|
Phosphatase
|
Neurological Disease
|
|
Licoflavone A is a flavonoid isolated from the roots of Glycyrrhiza uralensis, inhibits protein tyrosine phosphatase-1B (PTP1B), with an IC50 of 54.5 μM .
|
-
- HY-126319
-
|
|
VEGFR
EGFR
|
Cancer
|
|
SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively .
|
-
- HY-118144
-
|
|
BCRP
Src
|
Cancer
|
|
PD166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, with IC50s of 6 nM and 8 nM for Src and Abl, respectively. PD166326 exhibits antileukemic activity .
|
-
- HY-147784
-
|
|
Btk
|
Cancer
|
|
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
|
-
- HY-153012
-
|
|
TAM Receptor
c-Fms
|
Cancer
|
|
Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with Kds of <0.1 μM .
|
-
- HY-147316A
-
|
|
Others
|
Cancer
|
|
TP-5801 TFA is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity .
|
-
- HY-15772S3
-
|
asandeutertinibum; Osimertinib-d3; AZD-9291-d3
|
EGFR
|
Cancer
|
|
Asandeutertinib (Osimertinib-d3; AZD-9291-d3) is a epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, with antineoplastic effect .
|
-
- HY-19909A
-
|
|
EGFR
|
Cancer
|
|
NRC-2694-A is an orally effective EGFR tyrosine kinase inhibitor. NRC-2694-A can be used in the study of malignant squamous cell carcinoma (HNSCC) .
|
-
- HY-142512
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .
|
-
- HY-123856
-
|
|
Phosphatase
|
Neurological Disease
|
|
MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 attenuates binge-like ethanol consumption and ethanol reward .
|
-
- HY-148228
-
|
|
ROS Kinase
|
Cancer
|
|
ROS kinases-IN-1 (pag 98) is a ROS tyrosine kinase inhibitor with IC50 value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity .
|
-
- HY-152849A
-
|
HL5101 oxalate
|
c-Met/HGFR
|
Cancer
|
|
Boditrectinib oxalate is a potent tyrosine kinase inhibitor. Boditrectinib oxalate serves as an antineoplastic agent. Boditrectinib oxalate is useful in the research of cancer, inflammation, neurodegenerative diseases and certain infectious diseases .
|
-
- HY-N12736
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Dehydrodanshenol A is a non-competitive inhibitor of Protein tyrosine phosphatase 1B (PTP1B), with an IC50 value of 8.5 μM. Dehydrodanshenol A can be used in diabetes-related research .
|
-
- HY-N0198R
-
|
|
Lipoxygenase
Autophagy
Ferroptosis
|
Neurological Disease
Cancer
|
|
Nordihydroguaiaretic acid (Standard) is the analytical standard of Nordihydroguaiaretic acid. This product is intended for research and analytical applications. Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8 μM) and tyrosine kinase inhibitor.
|
-
- HY-15463S
-
|
STI571-d8; CGP-57148B-d8
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib-d8 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
|
-
- HY-15463S1
-
|
STI571 d4; CGP-57148B d4
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib-d4 is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
|
-
- HY-110026
-
|
|
FLT3
|
Cancer
|
|
GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. GTP-14564 inhibits FLT3 ligand-dependent growth in Ba/F3 leukemia cells .
|
-
- HY-N12041
-
|
|
TAM Receptor
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
|
-
- HY-156659
-
|
|
Phosphatase
|
Others
|
|
NC1 is a noncompetitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 inhibits LYP by restricting the movement of the WPD-loop. NC1 inhibits LYP-mediated TCR signaling in T cells .
|
-
- HY-118304A
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6?nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC50=1?μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML) .
|
-
- HY-W015007
-
|
|
COX
|
Cardiovascular Disease
|
|
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity . Metyrosine is a very effective agent for blood pressure control .
|
-
- HY-134046
-
|
Isodocarpin
|
Melanocortin Receptor
|
Metabolic Disease
|
|
(-)-Isodocarpin (Isodocarpin), a diterpenoid, is a potent melanogenesis inhibitor with an IC50 of 0.19 μM in B16 4A5 cells. (-)-Isodocarpin inhibits the expression of tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA .
|
-
- HY-162427
-
|
|
Syk
|
Endocrinology
|
|
NMS-0963 (compound 1) is an inhibitor of spleen tyrosine kinase (SYK) with an oral activity and IC50 value of 3 nM. NMS-0963 inhibits BaF3-TEL/SYK cell line proliferative at 27 nM .
|
-
- HY-103032
-
|
|
PDGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl .
|
-
- HY-13524
-
-
- HY-13979
-
|
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM) .
|
-
- HY-19730
-
|
HM61713; BI 1482694
|
EGFR
|
Cancer
|
|
Olmutinib (HM61713; BI-1482694) is an orally active and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC .
|
-
- HY-12297
-
|
Surufatinib; HMPL-012
|
FGFR
VEGFR
|
Cancer
|
|
Sulfatinib (Surufatinib) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
|
