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ERK5 inhibitor

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標的別:	ERK (22) Apoptosis (2) Autophagy (1) Bcl-2 Family (1) CaMK (1) Caspase (1) Epigenetic Reader Domain (1) Ferroptosis (2) MEK (3) mTOR (1) p62 (1) Reactive Oxygen Species (ROS) (2) Reference Standards (2) TNK1 (1)
研究分野別:	Cancer (21) Cardiovascular Disease (1) Inflammation/Immunology (2) Metabolic Disease (1)

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Targets Recommended: ERK

製品番号	製品名	Target	研究分野	構造式

HY-12056

BIX02189 5+ Cited Publications	MEK ERK	Cancer
BIX02189 is a potent and selective MEK5 inhibitor with an IC₅₀ of 1.5 nM. BIX02189 also inhibits *ERK5* catalytic activity with an IC₅₀ of 59 nM.

HY-14443

XMD8-92 Maximum Cited Publications 15 Publications Verification	Epigenetic Reader Domain ERK TNK1 CaMK	Cancer
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with K_ds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with K_ds of 190, 600 and 890 nM, respectively. Anti-cancer activity .

HY-128341

ERK5-IN-2	ERK	Cardiovascular Disease Cancer
ERK5-IN-2 is an orally active, sub-micromolar, selective *ERK5* inhibitor with IC₅₀s of 0.82 μM, 3 μM for *ERK5* and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .

HY-108886

JWG-071 5 Publications Verification	ERK	Cancer
JWG-071 is the kinase-selective chemical probe for *ERK5. JWG-071 inhibits* ERK5 and LRRK2 with IC₅₀ values of 88nM and 109 nM, respectively .

HY-14403

ERK5-IN-1	ERK	Cancer
ERK5-IN-1 is a potent *ERK5* inhibitor with an IC₅₀ of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC₅₀ of 26 nM.

HY-15665

XMD17-109 5+ Cited Publications	ERK	Cancer
XMD17-109 is a novel, specific *ERK-5* inhibitor, with an IC₅₀ of 162 nM.

HY-101846

AX-15836 5+ Cited Publications	ERK	Inflammation/Immunology Cancer
AX-15836 is a potent and selective *ERK5* inhibitor with an IC₅₀ of 8 nM.

HY-12055

BIX02188 3 Publications Verification	MEK ERK	Cancer
BIX02188 is a potent MEK5-selective inhibitor with an IC₅₀ of 4.3 nM. BIX02188 inhibits *ERK5* catalytic activity, with an IC₅₀ of 810 nM.

HY-112082

BAY885 1 Publications Verification	ERK	Cancer
BAY885, a chemical probe, is a highly potent and selective *ERK5* inhibitor with an IC₅₀ of 35 nM. BAY885 shows weak inhibition on others kinases .

HY-156450

ERK5-IN-5	ERK	Cancer
ERK5-IN-5 (compound 4a) is an *ERK5* kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC₅₀ value of 6.23 µg/mL for A549 cells .

HY-173119

SKLB-D18	ERK Autophagy Apoptosis p62 mTOR Reactive Oxygen Species (ROS) Ferroptosis	Cancer
SKLB-D18 is an orally active *ERK1/2/ERK5* inhibitor, with an IC₅₀ of 38.69 nM and a K_d of 126.9 nM against human ERK1, an IC₅₀ of 40.12 nM and a K_d of 209.8 nM against ERK2, and an IC₅₀ of 59.72 nM and a K_d of 468.2 nM against *ERK5. SKLB-D18 inhibits* cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of *p-ERK5, p-RSKp90, p-c-Myc* and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer .

HY-149412

MHJ-627	ERK	Cancer
MHJ-627 is a potent *ERK5* (MAPK7) inhibitor (IC₅₀: 0.91 μM). MHJ-627 promotes the mRNA expression of tumor suppressors and anti-metastatic genes, and promotes cancer cell death .

HY-107622

(E/Z)-BIX02188	ERK MEK	Metabolic Disease
(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .

HY-156451

ERK5-IN-6	ERK	Cancer
ERK5-IN-6 (compound 5J) is an *ERK5* kinase inhibitor with anticancer activity. ERK5-IN-6 exhibits good anti-proliferative activity with the IC₅₀ value of 4.56 µg/mL for A549 cells .

HY-150606

ERK5-IN-4	ERK	Cancer
ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits *ERK5* (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC₅₀ of 77 nM and 300 nM, respectively .

HY-150605

ERK5-IN-3	ERK	Cancer
ERK5-IN-3 (compound 33j) is a potent and selective *ERK5* (extracellular signal-related kinase 5) inhibitor, with an IC₅₀ of 6 nM. ERK5-IN-3 shows antiproliferation activity against Hela cells, with an IC₅₀ of 31 nM .

HY-138215

ADTL-EI1712	ERK	Cancer
ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and *ERK5*, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .

HY-181477

ERK5-IN-7	ERK Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species (ROS)	Cancer
ERK5-IN-7 is an orally active *ERK5* inhibitor with an IC₅₀ of 403.4 nM. ERK5-IN-7 directly inhibits *ERK5* kinase activity, and downregulates the phosphorylation level and total protein expression of *ERK5. ERK5-IN-7* induces Apoptosis (upregulates Bax, downregulates Bcl-2, and induces Caspase-3 cleavage). ERK5-IN-7 induces ROS accumulation. ERK5-IN-7 exhibits anticancer effects against Lewis lung cancer .

HY-181968

JWG-045	ERK Ferroptosis	Cancer
JWG-045 is a selective *ERK5* inhibitor. JWG-045 exhibits unique ferroptosis-resistant activity independent of ERK5 inhibition. JWG-045 can be used in breast cancer research .

HY-108886R

JWG-071 (Standard)	Reference Standards ERK	Cancer
JWG-071 (Standard) is the analytical standard of JWG-071 (HY-108886). This product is intended for research and analytical applications. JWG-071 is the K_inase-selective chemical probe for ERK5. JWG-071 inhibits ERK5 and LRRK2 with IC₅₀ values of 88nM and 109 nM, respectively .

HY-101846R

AX-15836 (Standard)	Reference Standards ERK	Inflammation/Immunology Cancer
AX-15836 (Standard) is the analytical standard of AX-15836 (HY-101846). This product is intended for research and analytical applications. AX-15836 is a potent and selective ERK5 inhibitor with an IC₅₀ of 8 nM.

HY-182398

BAY-693	ERK	Cancer
BAY-693 is a highly potent and highly selective *ERK5* inhibitor with an IC₅₀ of 6.40 μM. BAY-693 reduces the transcriptional activity of MEF2. BAY-693 is applicable for cancer research .

製品番号	製品名

HY-L010

MAPK Compound Library	1,063 compounds
MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers. MCE designs a unique collection of 1,063 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

MAPK Compound Library

1,063 compounds

MAPK families play an important role in complex cellular programs like proliferation, differentiation, development, transformation, and apoptosis. In mammalian cells, four MAPK families have been clearly characterized: ERK1/2, C-Jun N-terminal kinse/stress-activated protein kinase (JNK/SAPK) , p38 kinase and ERK5. They respond to different signals. Each MAPK-related cascade consists of three enzymes that are activated in series: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK) and a MAP kinase (MAPK). MAPK signaling pathways has been implicated in the development of many human diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS) and various types of cancers.

MCE designs a unique collection of 1,063 MAPK signaling pathway inhibitors that act as a useful tool for MAPK-related drug screening and disease research.

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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