Search Result

Results for "

A375

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Cytotoxin (1) Antibiotic (1) Apoptosis (18) Aquaporin (1) Bacterial (1) Bcr-Abl (1) Caspase (1) CDK (3) CRM1 (1) Cytochrome P450 (1) DGK (1) Dihydroorotate Dehydrogenase (2) DNA/RNA Synthesis (4) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (1) Early 2 Factor (E2F) (1) Endogenous Metabolite (2) Epigenetic Reader Domain (1) ERK (8) FAK (2) Ferroptosis (1) FGFR (1) FLT3 (1) HBV (1) HDAC (2) Histone Methyltransferase (3) IAP (2) JAK (1) Ligands for Target Protein for PROTAC (1) MDM-2/p53 (2) MEK (8) Melanocortin Receptor (1) Microtubule/Tubulin (2) Necroptosis (1) NF-κB (1) Nucleoside Antimetabolite/Analog (1) Organoid (1) p38 MAPK (2) p62 (1) Parasite (1) PARP (1) PD-1/PD-L1 (1) PERK (2) PGE synthase (1) PI3K (2) PROTACs (5) Proteasome (1) Raf (9) Reactive Oxygen Species (2) Sirtuin (1) Src (1) STAT (2) Toll-like Receptor (TLR) (1) Topoisomerase (1) Tyrosinase (1) VEGFR (1)
By Research Areas:	Cancer (67) Infection (1) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (1)

By Targets:

ADC Cytotoxin (1)

Antibiotic (1)

Apoptosis (18)

Aquaporin (1)

Bacterial (1)

Bcr-Abl (1)

Caspase (1)

CDK (3)

CRM1 (1)

Cytochrome P450 (1)

DGK (1)

Dihydroorotate Dehydrogenase (2)

DNA/RNA Synthesis (4)

Drug-Linker Conjugates for ADC (1)

E1/E2/E3 Enzyme (1)

Early 2 Factor (E2F) (1)

Endogenous Metabolite (2)

Epigenetic Reader Domain (1)

ERK (8)

FAK (2)

Ferroptosis (1)

FGFR (1)

FLT3 (1)

HBV (1)

HDAC (2)

Histone Methyltransferase (3)

IAP (2)

JAK (1)

Ligands for Target Protein for PROTAC (1)

MDM-2/p53 (2)

MEK (8)

Melanocortin Receptor (1)

Microtubule/Tubulin (2)

Necroptosis (1)

NF-κB (1)

Nucleoside Antimetabolite/Analog (1)

Organoid (1)

p38 MAPK (2)

p62 (1)

Parasite (1)

PARP (1)

PD-1/PD-L1 (1)

PERK (2)

PGE synthase (1)

PI3K (2)

PROTACs (5)

Proteasome (1)

Raf (9)

Reactive Oxygen Species (2)

Sirtuin (1)

Src (1)

STAT (2)

Toll-like Receptor (TLR) (1)

Topoisomerase (1)

Tyrosinase (1)

VEGFR (1)

By Research Areas:

Cancer (67)

Infection (1)

Inflammation/Immunology (3)

Metabolic Disease (2)

Neurological Disease (1)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-128224

Antiproliferative agent-13	Others	Cancer
Antiproliferative agent-13 (compound 16c) shows an antiproliferative activity against human A375 cells with an IC₅₀ value of 32.7 nM. Antiproliferative agent-13 can be used for the research of cancer .

HY-N10335

Harringtonolide 1 Publications Verification	FAK	Inflammation/Immunology Cancer
Harringtonolide is a potent RACK1 inhibitor (IC₅₀=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .

HY-N3838

Epitulipinolide diepoxide	Others	Cancer
Epitulipinolide diepoxide (compound 9) is a natural compound isolated from the herbs of Liriodendron chinense (Hemsl.) Sarg. Epitulipinolide diepoxide displays cytoxicity in A375 cells, with the IC₅₀ of 52.03 μM .

HY-120607

Chevalone C	Parasite	Infection Cancer
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC₅₀ value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .

HY-158027

B-Raf IN 17	Raf VEGFR FGFR	Cancer
B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAF_WT, VEGFR-2, and FGFR-1 in A375 cell line, with IC₅₀ values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer .

HY-153864

PROTAC MEK1 Degrader-1	PROTACs MEK ERK	Cancer
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC₅₀ value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .

HY-153445A

MEK-IN-6 hydrate

MEK Cancer

MEK-IN-6 hydrate (compound 69) is a MEK inhibitor. MEK-IN-6 hydrate has an IC₅₀ of 2 nM for A375 cells .
HY-153469

Benzyl DC-81

ADC Cytotoxin Cancer

Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
HY-16667

HLM006474

3 Publications Verification

Early 2 Factor (E2F) Cancer

HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC₅₀ of 29.8 µM in A375 cells.

MEK-IN-6 hydrate	MEK	Cancer
MEK-IN-6 hydrate (compound 69) is a MEK inhibitor. MEK-IN-6 hydrate has an IC₅₀ of 2 nM for A375 cells .

Benzyl DC-81	ADC Cytotoxin	Cancer
Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .

HLM006474 3 Publications Verification	Early 2 Factor (E2F)	Cancer
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC₅₀ of 29.8 µM in A375 cells.

HY-144271

RAF-IN-1	Raf	Cancer
RAF-IN-1 is a potent b/cRAF inhibitor with an IC₅₀s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF ^wt, and bRAF ^V600E. RAF-IN-1 shows cell growth inhibition with GI₅₀s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF ^V600E mutation, respectively .

HY-144269

SHR902275	Raf	Cancer
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC₅₀s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF ^wt, and bRAF ^V600E, respectively. SHR902275 shows cell growth inhibition with GI₅₀s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .

HY-122506

Salviolone	STAT	Cancer
Salviolone is a natural diterpenoid derivative that can against melanoma cells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells .

HY-153738

ERK1/2 inhibitor 9	ERK	Cancer
ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .

HY-153341

CFT1946	PROTACs Raf	Cancer
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ^™) degrader of BRAF ^V600E with a DC₅₀ of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF ^V600E splice variant. CFT1946 can be used in tumor research .

HY-13323

CX-5461 25+ Cited Publications	DNA/RNA Synthesis	Cancer
CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC₅₀s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .

HY-13323A

CX-5461 dihydrochloride 25+ Cited Publications	DNA/RNA Synthesis	Cancer
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC₅₀s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC₅₀ ≥25 μM).

HY-153445

MEK-IN-6	ERK MEK	Cancer
MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC₅₀: 2 nM). MEK-IN-6 can be used for research of cancer .

HY-N0201

Atractylenolide I 2 Publications Verification	Toll-like Receptor (TLR) JAK STAT	Cancer
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.

HY-12842

UC-112	IAP Apoptosis	Cancer
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).

HY-147788

hDHODH-IN-9	Dihydroorotate Dehydrogenase	Cancer
hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC₅₀ of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .

HY-15816A

Ulixertinib hydrochloride 20+ Cited Publications BVD-523 hydrochloride; VRT752271 hydrochloride	ERK	Cancer
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

HY-15610

GDC-0623 5+ Cited Publications RG 7421; MEK inhibitor 1	MEK Apoptosis	Cancer
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (K_i=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC₅₀=42 nM) versus A375 (BRAF ^V600E, EC₅₀=7 nM).

HY-147734

Calpain Inhibitor-2	Others	Cancer
Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.

HY-15816

Ulixertinib 20+ Cited Publications BVD-523; VRT752271	ERK	Cancer
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .

HY-P1726A

MSG606 TFA	Melanocortin Receptor
MSG606 TFA is a potent human MC1 receptor antagonist (IC₅₀=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC₅₀ values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.

HY-138098

Sartorypyrone B	Others	Cancer
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI₅₀s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .

HY-B0078

Dacarbazine 5+ Cited Publications Imidazole Carboxamide	Nucleoside Antimetabolite/Analog Apoptosis	Cancer
Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC₅₀ of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma .

HY-126288

ASTX029

4 Publications Verification

ERK Apoptosis Cancer

ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC₅₀: 2.7 nM). ASTX029 has anti-cancer activity .

ASTX029 4 Publications Verification	ERK Apoptosis	Cancer
ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC₅₀: 2.7 nM). ASTX029 has anti-cancer activity .

HY-149005

PRMT5-IN-19	Histone Methyltransferase	Cancer
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC₅₀ values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .

HY-147731

HDAC6-IN-9	HDAC	Cancer
HDAC6-IN-9 (compound 12c) is a potent and selective HDAC6 inhibitor with IC₅₀ values of 11.8, 15.2, 4.2, 139.6, 21.3 nM for HDAC1,HDAC3, HDAC6, HDAC8, HDAC10, respectively. HDAC6-IN-9 shows anti-proliferative activities .

HY-148059

Uplarafenib

B-Raf IN 10
Raf Cancer

Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC₅₀ between 50 and 100 nM. Uplarafenib shows antitumor activity .

Uplarafenib B-Raf IN 10	Raf	Cancer
Uplarafenib (B-Raf IN 10) (Compound C09) is a BRAF inhibitor with an IC₅₀ between 50 and 100 nM. Uplarafenib shows antitumor activity .

HY-155571

MDM2/XIAP-IN-3	MDM-2/p53 IAP	Cancer
MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death .

HY-163356

Tubulin polymerization-IN-60	Microtubule/Tubulin Apoptosis	Cancer
Tubulin polymerization-IN-60 (BF3) is a tubulin polymerization inhibitor with anticancer activity. Tubulin polymerization-IN-60 (BF3) belongs to the colchicine binding site inhibitors (CBSIs) and disturbs cell cycle progression leading to G2/M arrest and apoptosis .

HY-B1139

Tolperisone hydrochloride 1 Publications Verification	Apoptosis	Neurological Disease
Tolperisone hydrochloride is a centrally acting muscle relaxant studied in neurological disorders causing pathological rhabdomyosclerosis (pyramidal tract injury, multiple sclerosis, myelopathy, encephalomyelitis), spastic paralysis, and other muscle dystonia-related Encephalopathy. Tolperisone hydrochloride also has antiviral activity .

HY-112089

Naporafenib 2 Publications Verification LXH254	Raf p38 MAPK Bcr-Abl	Cancer
Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC₅₀ values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .

HY-N4187

Licochalcone D 1 Publications Verification	NF-κB Apoptosis Reactive Oxygen Species	Metabolic Disease Inflammation/Immunology Cancer
Licochalcone D, a flavonoid compound mainly existing in the root of Glycyrrhiza uralensis, is a potent and orally active inhibitor of NF-kappaB (NF-κB) p65. Licochalcone D possesses antioxidant, anti-inflammatory, anti-cancer properties .

HY-117996

KPT-251	CRM1 Apoptosis	Cancer
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity .

HY-149616

PPM-3	PROTACs ERK	Cancer
PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC₅₀ of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .

HY-157800

Trilexium TRX-E-009-1	Microtubule/Tubulin Apoptosis PARP Caspase	Cancer
Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity .

HY-12970A

EPZ020411 hydrochloride 5 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC₅₀ of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer .

HY-N0351

p-Coumaric acid 1 Publications Verification trans-4-Hydroxycinnamic acid	Endogenous Metabolite Bacterial Apoptosis	Inflammation/Immunology Cancer
p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .

HY-12970

EPZ020411 5 Publications Verification	Histone Methyltransferase Apoptosis	Cancer
EPZ020411 is a selective inhibitor of PRMT6 with an IC₅₀ of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer .

HY-12847

CCT241161	Raf Src Apoptosis	Cancer
CCT241161 is an orally active pan-RAF inhibitor with IC₅₀s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .

HY-143270

PROTAC BRD9-binding moiety 5	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
PROTAC BRD9-binding moiety 5 is a selective BRD9 binder with an IC₅₀ value of 4.20 μM, can be used for the synthesis of PROTACs. PROTAC BRD9-binding moiety 5 has antiproliferative activity against cancer cells .

HY-137487

PROTAC BRAF-V600E degrader-1	PROTACs Raf	Cancer
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with K_d value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth .

HY-155874

ZNL-05-044	CDK	Cancer
ZNL-05-044 is a CDK11 inhibitor with an IC₅₀s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing .

HY-129180

XY028-133

PROTACs CDK Cancer

XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK .

HY-144692

MEK/PI3K-IN-1	MEK PI3K PERK	Cancer
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .

HY-144693

MEK/PI3K-IN-2	MEK PI3K PERK	Cancer
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC₅₀ values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .

HY-146029

Apoptosis inducer 3	Apoptosis	Cancer
Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks