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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

A375 cells

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Cytotoxin (1) Apoptosis (4) Aquaporin (1) CDK (1) DGK (1) Dihydroorotate Dehydrogenase (1) DNA/RNA Synthesis (3) Early 2 Factor (E2F) (1) Endogenous Metabolite (1) ERK (6) FAK (1) FGFR (1) HBV (1) HDAC (1) Histone Methyltransferase (1) IAP (1) JAK (1) MEK (4) Melanocortin Receptor (1) Microtubule/Tubulin (1) Organoid (1) Parasite (1) PD-1/PD-L1 (1) PROTACs (2) Raf (4) Sirtuin (1) STAT (2) Toll-like Receptor (TLR) (1) VEGFR (1)
By Research Areas:	Cancer (34) Infection (1) Inflammation/Immunology (1)

By Targets:

ADC Cytotoxin (1)

Apoptosis (4)

Aquaporin (1)

CDK (1)

DGK (1)

Dihydroorotate Dehydrogenase (1)

DNA/RNA Synthesis (3)

Early 2 Factor (E2F) (1)

Endogenous Metabolite (1)

ERK (6)

FAK (1)

FGFR (1)

HBV (1)

HDAC (1)

Histone Methyltransferase (1)

IAP (1)

JAK (1)

MEK (4)

Melanocortin Receptor (1)

Microtubule/Tubulin (1)

Organoid (1)

Parasite (1)

PD-1/PD-L1 (1)

PROTACs (2)

Raf (4)

Sirtuin (1)

STAT (2)

Toll-like Receptor (TLR) (1)

VEGFR (1)

By Research Areas:

Cancer (34)

Infection (1)

Inflammation/Immunology (1)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Targets Recommended: Nuclear Factor of activated T Cells (NFAT)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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 .

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 .

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-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.

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-B0150

Nicotinamide Maximum Cited Publications 36 Publications Verification Niacinamide; Nicotinic acid amide	Organoid Endogenous Metabolite Sirtuin HBV	Cancer
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC₅₀: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD₊, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity .

HY-148174

JNJ-3790339	DGK	Cancer
JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC₅₀ of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .

HY-P99115

Envafolimab ASC 22; KN 035	PD-1/PD-L1	Cancer
Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC₅₀ value of 5.25 nM. Envafolimab has the potential for the research of solid tumors .

HY-147356

ERCC1-XPF-IN-2	DNA/RNA Synthesis	Cancer
ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC₅₀ value of 0.6 µM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays .

HY-145702

MAP855	MEK ERK	Cancer
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC₅₀=3 nM, pERK EC₅₀=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .

HY-148713

Anti-CSCs agent-1	Apoptosis	Cancer
Anti-CSCs agent-1 is a potent anti-CSCs agent. Anti-CSCs agent-1 inhibits cell growth and cell migration. Anti-CSCs agent-1 induces Apoptosis. Anti-CSCs agent-1 inhibits the viability of CSCs. Anti-CSCs agent-1 enhances the production of ROS in CSCs. Anti-CSCs agent-1 shows antitumor activity .

HY-157979

AQP3-IN-1

Aquaporin Cancer

AQP3-IN-1 (compounds 3) is an AQP3 inhibitor with a IC₅₀ value of 8.91 μM. AQP3-IN-1 inhibits cell proliferation of melanoma cells .

AQP3-IN-1	Aquaporin	Cancer
AQP3-IN-1 (compounds 3) is an AQP3 inhibitor with a IC₅₀ value of 8.91 μM. AQP3-IN-1 inhibits cell proliferation of melanoma cells .

HY-146276

CDK/HDAC-IN-2	HDAC CDK Apoptosis	Cancer
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC₅₀ of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .

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.

Envafolimab ASC 22; KN 035	PD-1/PD-L1	Cancer
Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC₅₀ value of 5.25 nM. Envafolimab has the potential for the research of solid tumors .

Harringtonolide 1 Publications Verification	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Cephalotaxus harringtonia Plants Cephalotaxaceae Inflammation/Immunology Disease Research Fields Cancer	FAK
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 .

Salviolone	Structural Classification Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	STAT
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 .

Atractylenolide I 2 Publications Verification	Structural Classification Classification of Application Fields Terpenoids Sesquiterpenes Source classification Astragalus caprinus L. Plants Compositae Disease Research Fields Cancer	Toll-like Receptor (TLR) JAK STAT
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.

Chevalone C	Infection Triterpenes Microorganisms Classification of Application Fields Terpenoids Source classification Disease Research Fields	Parasite
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 .

Epitulipinolide diepoxide	Structural Classification Natural Products Source classification Magnoliaceae Liriodendron tulipifera L. Plants	Others
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 .

Sartorypyrone B	Triterpenes Microorganisms Classification of Application Fields Terpenoids Source classification Disease Research Fields Cancer	Others
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 .

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