Search Result

Results for "

kinome

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (3) Aminotransferases (Transaminases) (1) Apoptosis (3) Bcr-Abl (1) c-Fms (2) c-Kit (2) Casein Kinase (1) CDK (1) Cyclophilin (1) DYRK (1) EGFR (6) ERK (1) FGFR (1) GSK-3 (1) Interleukin Related (1) Ligands for Target Protein for PROTAC (1) LIM Kinase (LIMK) (1) MAP4K (1) mGluR (1) Microtubule/Tubulin (1) p38 MAPK (1) PDGFR (2) PERK (1) Ras (1) Src (1) Tau Protein (2) TLK (1) TNF Receptor (1) Trk Receptor (1) ULK (1)
By Research Areas:	Cancer (17) Inflammation/Immunology (2) Metabolic Disease (3) Neurological Disease (6)

By Targets:

Akt (3)

Aminotransferases (Transaminases) (1)

Apoptosis (3)

Bcr-Abl (1)

c-Fms (2)

c-Kit (2)

Casein Kinase (1)

CDK (1)

Cyclophilin (1)

DYRK (1)

EGFR (6)

ERK (1)

FGFR (1)

GSK-3 (1)

Interleukin Related (1)

Ligands for Target Protein for PROTAC (1)

LIM Kinase (LIMK) (1)

MAP4K (1)

mGluR (1)

Microtubule/Tubulin (1)

p38 MAPK (1)

PDGFR (2)

PERK (1)

Ras (1)

Src (1)

Tau Protein (2)

TLK (1)

TNF Receptor (1)

Trk Receptor (1)

ULK (1)

By Research Areas:

Cancer (17)

Inflammation/Immunology (2)

Metabolic Disease (3)

Neurological Disease (6)

Inhibitors & Agonists

Isotope-Labeled Compounds

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-129550

BI-4020	EGFR	Cancer
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC₅₀=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC₅₀=1 nM). BI-4020 also shows activity against EGFR wt (IC₅₀=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .

HY-162426

UNC-CA2-103	TLK	Cancer
UNC-CA2-103 is a TLK2 inhibitor with a human IC₅₀ of 18 nM, and it exhibits high selectivity over TLK1 and the vast majority of other kinases. UNC-CA2-103 can be used in research related to breast cancer, glioblastoma and gastric cancer .

HY-12443

PF-5006739	Casein Kinase	Neurological Disease
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC₅₀s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .

HY-172429

Enozertinib ORIC-114	EGFR	Neurological Disease Cancer
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .

HY-122630

TH-257 1 Publications Verification	LIM Kinase (LIMK)	Cancer
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC₅₀ values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM .

HY-135805

JBJ-04-125-02	EGFR	Cancer
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC₅₀ of 0.26 nM for EGFR ^L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR ^{L858R/T790M/C797S} signaling. JBJ-04-125-02 has anti-tumor activities .

HY-138742

HPK1-IN-7	MAP4K	Cancer
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC₅₀=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .

HY-172429A

Enozertinib hemihydrate ORIC-114 hemihydrate	EGFR	Neurological Disease Cancer
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .

HY-15985

CTX-0294885 3 Publications Verification	Akt	Metabolic Disease Inflammation/Immunology Cancer
CTX-0294885 is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .

HY-153244

MFH290 1 Publications Verification	CDK	Cancer
MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .

HY-15985A

CTX-0294885 hydrochloride 3 Publications Verification	Akt	Metabolic Disease Inflammation/Immunology Cancer
CTX-0294885 hydrochloride is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .

HY-151903S

FGFR2/3-IN-1	FGFR	Cancer
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC₅₀s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC₅₀s of 2.7 nM and 6.1 nM, respectively .

HY-146697

IHMT-TRK-284	Trk Receptor c-Fms PDGFR Bcr-Abl c-Kit Apoptosis	Cancer
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC₅₀ values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .

HY-172544

TTBK1/2-IN-3	Tau Protein	Neurological Disease
TTBK1/2-IN-3 (Compound 10) is a potent inhibitor of tau tubulin kinase 1 (TTBK1) and TTBK2, with IC₅₀ values of 579 nM and 258 nM, respectively. TTBK1/2-IN-3 inhibits the phosphorylation of TDP-43. TTBK1/2-IN-3 reduces the expression of primary cilia on the surface of iPSCs .

HY-146262

LDC0496	EGFR	Cancer
LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .

HY-182043

BLU-654	c-Kit PDGFR	Cancer
BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT ^V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT ^V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors .

HY-183584

ARN25699	GSK-3 Src DYRK Tau Protein Microtubule/Tubulin	Neurological Disease
ARN25699 is a kinase inhibitor with an IC₅₀ of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies .

HY-103566A

LY456236 free base	mGluR EGFR p38 MAPK Apoptosis	Neurological Disease
LY456236 free base is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC₅₀ of 0.145 μM. LY456236 free base can also inhibit EGFR, with an IC₅₀ of 0.918 μM. LY456236 free base blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 free base can be used in epilepsy research .

HY-125142

AP-24567	Ligands for Target Protein for PROTAC	Cancer
AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342) .

HY-183569

CSF1R-IN-27	c-Fms Akt PERK Aminotransferases (Transaminases) Apoptosis TNF Receptor Interleukin Related	Metabolic Disease
CSF1R-IN-27 is a CSF1R inhibitor with oral effectiveness, kinome-wide selective profile, low cellular cytotoxicity, and CSF1R IC₅₀ values of 19 nM, 88 nM, 173 nM, 797 nM, 1448 nM, and >3000 nM. CSF1R-IN-27 suppresses M-CSF-induced phosphorylation of CSF1R, AKT, and ERK in macrophages, and inhibits hepatic p-CSF1R/p-AKT/p-ERK signaling. CSF1R-IN-27 reduces serum transaminase levels, improves hepatic histopathology, alleviates inflammatory cell infiltration, and decreases circulating TNF-α and IL-6 levels. CSF1R-IN-27 can be used for the research of acute liver injury .

HY-181699

ULK1-IN-5	ULK	Cancer
ULK1-IN-5 (Compound D1) is a selective ULK1 inhibitor with an IC₅₀ of 14.91 nM. ULK1-IN-5 functionally inhibits the kinase activity of ULK1. ULK1-IN-5 reduces the phosphorylation level of ATG13. ULK1-IN-5 exerts antiproliferative effects on cervical cancer cells. ULK1-IN-5 is applicable to relevant research on cervical cancer .

HY-186087

RM-046	Ras ERK Cyclophilin	Cancer
RM-046 is an orally active, selective ternary complex inhibitor of KRAS ^Q61H (active form). RM-046 forms a ternary complex with cyclophilin A, binds to active KRAS ^Q61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRAS ^Q61H mutant cancers .

Cat. No.	Nombre del producto	Chemical Structure

HY-151903S

FGFR2/3-IN-1
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC₅₀s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC₅₀s of 2.7 nM and 6.1 nM, respectively .

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