Search Result
Results for "
A375 cell
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0150
-
Nicotinamide
Maximum Cited Publications
89 Publications Verification
Niacinamide; Nicotinic acid amide
|
Environmental Pollutants
Endogenous Metabolite
Sirtuin
HBV
Organoid
|
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-13323
-
|
|
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-15816
-
|
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-N0201
-
|
|
TNF Receptor
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-15816A
-
|
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-N0202
-
|
Asterolide
|
ERK
Apoptosis
p38 MAPK
Akt
Src
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
-
- HY-P99115
-
|
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-16667
-
|
|
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-153341
-
|
CFT1946
|
PROTACs
Raf
|
Cancer
|
|
Tagarafdeg (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. Tagarafdeg is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. Tagarafdeg can be used in tumor research .
|
-
-
- HY-122506
-
|
|
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-N10335
-
|
|
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-13323A
-
|
|
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-164781
-
-
-
- HY-N6843
-
-
-
- HY-153469
-
|
|
ADC Payload
|
Cancer
|
|
Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
|
-
-
- HY-Y1177
-
|
Phenyl disulfide
|
PI3K
Akt
mTOR
Ferroptosis
Apoptosis
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
|
Cancer
|
|
Diphenyl disulfide (Phenyl disulfide) is an organic disulfide compound. Diphenyl disulfide inhibits the PI3K/AKT/mTOR pathway, and induces ferroptosis (ferroptosis), apoptosis (apoptosis) and autophagy (autophagy) in cancer cells. Diphenyl disulfide downregulates GPX4 expression, inhibits NRF2 phosphorylation, induces lipid peroxidation, promotes xCT ubiquitination, induces proteolytic cleavage of p21 Bax into p18 Bax, and suppresses cell proliferation and viability. Diphenyl disulfide can be used in research related to melanoma and breast cancer .
|
-
-
- HY-12842
-
|
|
IAP
Survivin
Apoptosis
Caspase
|
Inflammation/Immunology
Cancer
|
|
UC-112 is a XIAP inhibitor with anticancer activity. UC-112 selectively downregulates and degrades survivin via the ubiquitin-mediated proteasomal degradation pathway. UC-112 reduces XIAP levels in in vivo tumor models. UC-112 activates caspase-3/7 and caspase-9, and induces cancer cell apoptosis. UC-112 is applicable to studies on melanoma, prostate cancer and cancer-related research .
|
-
-
- HY-118119
-
|
|
PGE synthase
YB-1
Apoptosis
JAK
STAT
TGF-β Receptor
TGF-beta/Smad
PI3K
Akt
|
Cancer
|
|
CAY10526 is an inhibitor of Y-box binding protein 1 (YB-1) and microsomal prostaglandin E2 synthase 1 (mPGES1). CAY10526 inhibits the production of PGE2 by suppressing YB-1 and mPGES1. CAY10526 induces cell apoptosis (apoptosis) and inhibits the JAK/STAT, TGF-β/Smad3 and PI3K/AKT signaling pathways. CAY10526 can be used in research related to melanoma, prostate cancer, esophageal adenocarcinoma, T-cell lymphoma, etc .
|
-
-
- HY-153864
-
|
|
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-176792
-
|
|
PROTACs
Ras
|
Cancer
|
|
ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRAS G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .
|
-
-
- HY-12291
-
|
HMSL 10017-101-1
|
Raf
Apoptosis
|
Cancer
|
|
HG6-64-1 (HMSL 10017-101-1) is a B-raf kinase modulator.HG6-64-1 modulates B-raf kinase activity, including the V600E mutant form and the drug-resistant gatekeeper mutation T529I. HG6-64-1 is a germinal center kinase inhibitor. HG6-64-1 induces cell cycle arrest and apoptosis. HG6-64-1 can be used for the research of diffuse large B-cell lymphoma (DLBCL) .
|
-
-
- HY-112462
-
|
|
CDK
|
Cancer
|
|
Cdk1/2 Inhibitor III (compound 3n) is a highly potent and selective Cdk1/cyclin B and Cdk2/cyclin A inhibitor of with IC50s of 0.6 nM and 0.5 nM, respectively. Cdk1/2 Inhibitor III shows selectivity over VEGF-R2 (IC50 of 32 nM), GSK-3β (IC50 of 140 nM), and a other kinases. Cdk1/2 Inhibitor III inhibits in cell proliferation with IC50s of 20 nM, 35 nM and 92 nM for HCT-116, HeLa, and A375 cells, respectively .
|
-
-
- HY-175370
-
|
|
PROTACs
RIP kinase
|
Cancer
|
|
PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373) .
|
-
-
- HY-153738
-
|
|
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-147356
-
|
|
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
-
|
|
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-161108
-
|
|
PROTACs
Checkpoint Kinase (Chk)
|
Cancer
|
|
PROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma .
|
-
-
- HY-101460
-
|
|
E3 Ligase Ligand-Linker Conjugates
Drug Derivative
|
Cancer
|
|
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .
|
-
-
- HY-128224
-
|
|
Drug Intermediate
|
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-153445
-
|
MEK-IN-6
|
ERK
MEK
|
Cancer
|
|
Polfurmetinib (MEK-IN-6) (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). Polfurmetinib can be used for research of cancer .
|
-
-
- HY-15816R
-
|
BVD-523 (Standard); VRT752271 (Standard)
|
ERK
Reference Standards
|
Cancer
|
|
Ulixertinib (Standard) is the analytical standard of Ulixertinib. This product is intended for research and analytical applications. 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-144269
-
|
|
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-179505
-
|
|
YAP
|
Cancer
|
|
OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research .
|
-
-
- HY-121255
-
|
(R)-Cryptopleurine; NSC 19912
|
TMV
|
Cancer
|
|
(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
|
-
-
- HY-163858
-
|
|
Haspin Kinase
|
Cancer
|
|
Haspin-IN-4 (Compound 60) is a selective inhibitor of Haspin with an IC50 value of 0.01 nM. Haspin-IN-4 possesses anticancer activity and can be used in cancer research .
|
-
-
- HY-144271
-
|
|
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-176508
-
|
|
Casein Kinase
|
Cancer
|
|
KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models .
|
-
-
- HY-16461
-
|
(-)-Solenopsin A
|
Akt
Ribosomal S6 Kinase (RSK)
PI3K
PDK-1
FOXO
Mitophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
|
Cardiovascular Disease
|
|
Solenopsin ((-)-Solenopsin A) is an ATP-competitive and selective Akt-1 inhibitor with an IC50 of 5-10 μM, and also acts as an RSK1 inhibitor. Solenopsin inhibits the activities of PDK1 in lipid rafts, downregulates PI3K, blocks PI3K-dependent generation of 3-phosphoinositides, and suppresses the phosphorylation of FOXO1a. Solenopsin induces Mitophagy and ROS production, reduces mitochondrial oxygen consumption, and exhibits antiproliferative and antiangiogenic activities. Solenopsin can be used in research related to hyperproliferative skin diseases and malignant diseases .
|
-
-
- HY-169086
-
|
|
PROTACs
|
Cancer
|
|
KL-465 is a MAGE-A3 PROTAC degrader that degrades MAGE-A3 in HeLa cells with a DC50 of 2 μM. KL-465 inhibits the proliferation of MAGE-A3-positive cancer cells. KL-465 can be used for the research of MAGE-A3-related cancers .
|
-
-
- HY-179717
-
|
|
PROTACs
Microphthalmia Associated Transcription Factor (MITF)
|
Cancer
|
|
WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces the MITF protein levels in several melanoma cell lines, including B16F10, A375, and GAK. WZS0347 significantly inhibits the proliferation, migration, and invasion of melanoma cells. WZS0347 can be used for research on melanoma (Pink: MITF ligand: (HY-179718); Blue: CRBN ligand: (HY-131717); Black: linker: (HY-22391)) .
|
-
-
- HY-177132
-
|
WX001
|
ERK
|
Cancer
|
|
Sonvuterkib (WX001) is a potent and orally active extracellular signal-regulated kinases (ERK) inhibitor with IC50 values of 1.4, 0.54 nM for ERK1, ERK2, respectively. Sonvuterkib inhibits cell proliferation. Sonvuterkib shows anticancer activity .
|
-
-
- HY-B0150A
-
|
Niacinamide hydrochloride; Nicotinic acid amide hydrochloride
|
Sirtuin
Endogenous Metabolite
HBV
|
Infection
Cancer
|
|
Nicotinamide hydrochloride is a form of vitamin B3 or niacin. Nicotinamide hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide hydrochloride also inhibits SIRT1. Nicotinamide hydrochloride increases cellular NAD+, ATP, ROS levels. Nicotinamide hydrochloride inhibits tumor growth and improves survival. Nicotinamide hydrochloride also has anti-HBV activity .
|
-
-
- HY-N3838
-
|
|
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-153735
-
|
|
PROTACs
ERK
|
Cancer
|
|
ERK-CLIPTAC is a ERK CLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer .
|
-
-
- HY-13323R
-
|
|
Reference Standards
DNA/RNA Synthesis
|
Cancer
|
|
CX-5461 (Standard) is the analytical standard of CX-5461. This product is intended for research and analytical applications. 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-177914
-
|
|
MEK
|
Cancer
|
|
MEK-IN-7 (compound WX086) is potent, orally active and selective MEK inhibitor (MEK1 IC50 = 29.62 nM). MEK-IN-7 inhibits HT29 and A375 cell proliferation with IC50s of 0.62 and 0.40 nM. MEK-IN-7 inhibits tumor growth in a HL-29 xenograft mouse model. MEK-IN-7 can be used for melanoma and colon cancer research .
|
-
-
- HY-120281
-
|
|
MEK
PI3K
Akt
Apoptosis
Caspase
|
Cancer
|
|
ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
|
-
-
- HY-120607
-
|
|
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-163595
-
|
|
Ras
|
Cancer
|
|
KRAS G12D-IN-31 is a potent KRAS G12D inhibitor with an IC50 of < 100 nM. KRAS G12D-IN-31 inhibits the proliferation of RAS-dependent cells (KRAS G12C, KRAS G12D, KRAS G12V and KRAS WT). KRAS G12D-IN-31 can be used to study non-small cell lung cancer, gastric cancer, colon cancer, and malignant melanoma .
|
-
-
- HY-162900
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-32 is a Hsp90 C-terminal inhibitor that displays anti-proliferative activities against SKMel173, SKMel103, SKMel19 and A375 cells with IC50 values of 1.01 μM, 0.782 μM, 0.607 μM and 1.413 μM , respectively. HSP90-IN-32 is promising for research of anti-cancer agents .
|
-
- HY-126214S
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .
|
-
- HY-148174
-
|
|
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-153445A
-
|
MEK-IN-6 hydrate
|
MEK
|
Cancer
|
|
Polfurmetinib (MEK-IN-6) hydrate (compound 69) is a MEK inhibitor. Polfurmetinib hydrate has an IC50 of 2 nM for A375 cells .
|
-
- HY-157979
-
|
|
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-161882
-
|
|
PROTACs
|
Cancer
|
|
PROTAC SMARCA2 degrader-8 (compound 1) is a potent SMARCA2 degrader with a DC50 of 28nM in A375 cells .
|
-
- HY-146276
-
|
|
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 .
|
-
- HY-163594
-
|
|
Ras
|
Cancer
|
|
K-Ras-IN-58 is a K-RAS inhibitor and shows inhibitory activity against KRASG12D, KRASG12C and KRAS WT. K-Ras-IN-58 inhibits proliferation of cancer cells .
|
-
- HY-169298
-
|
|
Ferroptosis
|
Cancer
|
|
Ferroptosis-IN-15 (compound 12) is a potent inhibitor of ferroptosis, with the EC50s of 0.76 and 0.67 μM in A375 cells and 786-O cells, respectively.Ferroptosis-IN-15 is a potential iron chelator and radical trapping antioxidant .
|
-
- HY-175828
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DHPS-IN-2 is an allosteric deoxyhypusine synthase (DHPS) inhibitor with an IC50 of 70 nM and a Kd of 26.4 μM. DHPS-IN-2 significantly suppresses melanoma cell migration and invasiveness in vitro and exhibits potent anti-tumor efficacy in an A375 cell zebrafish xenograft model. DHPS-IN-2 can be used for the study of melanoma .
|
-
- HY-147734
-
|
|
Calcium Channel
|
Cancer
|
|
Calpain Inhibitor-2 (compound 5) is a peptide inhibitor of μ-calpain (Ki=9 nM). Calpain Inhibitor-2 exhibits antiproliferative activity against melanoma cell lines (A-375 and B-16F1) and PC-3 prostate cancer cells in vitro .
|
-
- HY-147788
-
|
|
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-N7484
-
|
|
Fungal
|
Cancer
|
|
(−)-Voacangarine is an indole alkaloid, which exhibits cytotoxic effects against cancer cells HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 of 5~20 mg/mL. (−)-Voacangarine inhibits the cultivation of Saccharomyces cerevisiae wildtype and repair-deficient mutants .
|
-
- HY-117872
-
|
20-O-Acetylsartorypyrone D
|
Fungal
|
Infection
|
|
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
|
-
- HY-174800
-
|
|
Topoisomerase
|
Cancer
|
|
ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer .
|
-
- HY-126180
-
|
|
MEK
|
Cancer
|
|
BAY-866, a sulfamide campound, is an allosteric MEK1 inhibitor with an IC50 of 14 nM. BAY-866 inhibits cell growth of A375 (BRAF) and HCT116 (K-Ras) with IC50s of 13 nM and 277 nM, respectively. BAY-866 inhibits tumor growth in K-Ras-mutated A549 xenograft model .
|
-
- HY-174274
-
|
|
ERK
|
Cancer
|
|
ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAF V600E mutant cells (IC50=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma .
|
-
- HY-N12834
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
|
-
- HY-N0201R
-
|
|
TNF Receptor
Reference Standards
Toll-like Receptor (TLR)
JAK
STAT
|
Cancer
|
|
Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. 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-158027
-
|
|
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 BRAFWT, 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-N13739
-
|
|
Tyrosinase
|
Cancer
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
- HY-164474
-
|
|
MEK
|
Cancer
|
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-161628
-
|
|
Topoisomerase
|
Cancer
|
|
Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
|
-
- HY-138098
-
|
|
Endogenous Metabolite
|
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-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-178382
-
|
|
Raf
Bcr-Abl
P-glycoprotein
PERK
Apoptosis
|
Cancer
|
|
BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma .
|
-
- HY-149005
-
|
|
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
-
|
|
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-164039
-
|
|
Ras
|
Cancer
|
|
Talorasib (compound 1-2) has antitumor activity .
|
-
- HY-174128
-
|
|
ERK
Apoptosis
|
Cancer
|
|
Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor (IC50 values are 3.04 nM and 1.57 nM, respectively). Multi-target kinase-IN-5 significantly inhibits cancer cell proliferation, migration and invasion, and induces cell apoptosis and cell cycle arrest. Multi-target kinase-IN-5 inhibits the phosphorylation of ERK1/2 and downregulates the activity of its downstream substrate RSK to exert anti-tumor effects. Multi-target kinase-IN-5 can be used in cancer research .
|
-
- HY-148713
-
|
|
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-180329
-
|
|
Ligands for E3 Ligase
ERK
Raf
|
|
|
CG 858-Neg (compound 13) is a negative control for Thalidomide (HY-14658)-derived PROTAC degraders, targeting BRAF and BRAF V600E with Ki values of 9.5 nM and 14.4 nM, respectively. CG 858-Neg inhibits downstream ERK phosphorylation and suppresses BRAF V600E-driven melanoma (e.g., A375 cells, IC50=492 nM) and colorectal cancer (e.g., HT-29 cells, IC50=459 nM) cells. CG 858-Neg can be used in research related to melanoma and colorectal cancer .
|
-
- HY-171186
-
|
|
Drug Derivative
|
Cancer
|
|
EAPB0202 is an imidazolium and quinoxaline derivative. EAPB0202 shows significant cytotoxicity to A375 human melanoma cell line with an IC50 of 2.35 μM. EAPB0202 can be used in the study of cancer .
|
-
- HY-182538
-
|
|
MEK
|
Cancer
|
|
G-963 is an allosteric inhibitor of mitogen-activated protein kinase kinase (MEK) with a MEK1 IC50 of 0.012 μM. G-963 interacts with Ser212 of MEK and exhibits potent antiproliferative activity against HCT116 colon cancer cells (EC50 = 0.120 μM) and A375 melanoma cells (EC50 = 0.025 μM). G-963 can be used for the research of colon cancer, melanoma .
|
-
- HY-169409
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property .
|
-
- HY-123859
-
|
|
Casein Kinase
FLT3
CDK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .
|
-
- HY-181058
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Cyclopamine-COO-2-ethoxy-1,3-benzodioxole-O-C-Triazole-C5-AC is a drug-linker conjugate, with Cyclopamine (HY-17024) as its drug moiety. Cyclopamine-COO-2-ethoxy-1,3-benzodioxole-O-C-Triazole-C5-AC itself exhibits no significant anti-tumor activity. Cyclopamine-COO-2-ethoxy-1,3-benzodioxole-O-C-Triazole-C5-AC can be used for the synthesis of ADC molecules .
|
-
- HY-B0150G
-
|
Niacinamide; Nicotinic acid amide
|
Endogenous Metabolite
Sirtuin
HBV
|
Infection
Cancer
|
|
Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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-D3141
-
|
|
|
Cancer
|
|
DR probe is a "dual-key-and-lock" fluorescent probe designed based on the Resorufin (HY-123533) scaffold (Ex/Em = 647 nm/663-738 nm). DR probe can be sequentially activated by hydrogen peroxide to form the intermediate SR, which acts as a tyrosinase substrate to trigger a fluorescence turn-on signal. DR probe can distinguish normal melanocytes from melanoma cells. DR probe supports cell imaging and can be applied to mouse melanoma models to achieve melanoma diagnosis with higher accuracy and lower false-positive rates. DR probe is applicable to relevant research on melanoma .
|
-
- HY-181602
-
|
|
ATP Synthase
COX
Oxidative Phosphorylation
AMPK
|
Cancer
|
|
ATP Synthesis-IN-4 is a mitochondria-targeted small-molecule ligand that inhibits ATP synthesis. ATP Synthesis-IN-4 binds to mtDNA G4s in melanoma cells, thereby inducing changes in mitochondrial metabolism and inhibiting cell proliferation. ATP Synthesis-IN-4 suppresses the translation of key mitochondrial respiratory chain proteins (CYTB, ATP8, COX1, COX3, ND2) in melanoma cells, downregulates the expression of OXPHOS complexes, activates the phosphorylation of AMPK, and induces metabolic reprogramming to upregulate glycolysis. ATP Synthesis-IN-4 is applicable to relevant research on melanoma .
|
-
- HY-12970B
-
|
|
Histone Methyltransferase
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Cancer
|
|
EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma .
|
-
- HY-181726
-
|
|
PERK
P-glycoprotein
Apoptosis
|
Cancer
|
|
BRAFV600E/ABL2-IN-2 is a dual BRAFV 600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV 600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma .
|
-
- HY-181131
-
|
|
CDK
Apoptosis
|
Cancer
|
|
Anticancer agent 300 (compound P14) is a CCND1, CDK4, CDK6, and CCNE1 modulator, with anti-proliferative, cell-cycle modulatory, senescence-inducing, and apoptosis-inducing activity. Anticancer agent 300 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma .
|
-
- HY-18658B
-
|
NVP-HDM201 succinate; HDM201 succinate
|
MDM-2/p53
|
Cancer
|
|
Siremadlin (NVP-HDM201) succinate is an MDM2 inhibitor and cell cycle regulator. Siremadlin succinate blocks the p53-binding pocket of MDM2, inhibits MDM2-mediated ubiquitination and degradation of p53, thereby activating the p53 pathway in p53 wild-type cells. Siremadlin succinate can be used in the research of cutaneous melanoma .
|
-
- HY-181130
-
|
|
CDK
Apoptosis
|
Cancer
|
|
Anticancer agent 299 (compound P12) is a cell-cycle inhibitor, senescence inducer, apoptosis inducer, and antiproliferative agent. Anticancer agent 299 exhibits selective activity against cancer cells with minimal effects on non-tumoral chondrocyte cells at relevant concentrations. Anticancer agent 299 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma .
|
-
- HY-182780
-
|
|
Drug Derivative
|
Cancer
|
|
LSPN925 is an anticancer agent. LSPN925 exhibits cytotoxic and antiproliferative activities against tumor cells. LSPN925 has predicted oral bioavailability, low risks of hepatotoxicity and acute toxicity, and no risk of cardiotoxicity. LSPN925 can be used for the research of ovarian cancer, melanoma and breast cancer .
|
-
- HY-181545A
-
|
|
NO Synthase
IFNAR
|
Cancer
|
|
nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways .
|
-
- HY-183806
-
|
|
Others
|
Cancer
|
|
ANTXR1-IN-1 is a ANTXR1 inhibitor with a Ka of 2.88 μM for hANTXR1, and exhibits anti-tumor cell activity. ANTXR1-IN-1 undergoes acylation with Ser229 of ANTXR1, thereby inhibiting tumor cell proliferation. ANTXR1-IN-1 induces G2/M phase arrest and apoptosis in tumor cells. ANTXR1-IN-1 can be used for research on melanoma, non-small cell lung cancer, hepatocellular carcinoma, and colorectal cancer .
|
-
- HY-D3140
-
|
|
Fluorescent Dye
Tyrosinase
|
Cancer
|
|
MB-m-borate is a double-locked near-infrared fluorescence-activated probe (Ex/Em ≈ 647 nm/684 nm). MB-m-borate undergoes cascade activation by hydrogen peroxide and tyrosinase to release the fluorophore methylene blue, thereby generating a fluorescence activation response. MB-m-borate enables precise detection of melanoma in melanoma cells and mouse models. MB-m-borate can be used for melanoma research .
|
-
- HY-182899
-
|
|
PERK
Ras
COX
PD-1/PD-L1
Apoptosis
DNA/RNA Synthesis
Mitochondrial Metabolism
|
Cancer
|
|
DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma .
|
-
- HY-181529
-
|
|
VDAC
PERK
|
Cancer
|
|
NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2 and VDAC3. NCATS-SM0225 exhibits an IC50of 1.02 μM for ERAD and a Kd of 3.13 μM for human VDAC1 binding. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling and activating PERK. NCATS-SM0225 selectively kills cancer cells, exhibits tumor growth inhibitory effects in melanoma xenograft models. NCATS-SM0225 can be used for research on multiple cancers including melanoma, as well as the molecular mechanisms of ERAD and calcium homeostasis regulation .
|
-
- HY-156418
-
|
|
DNA/RNA Synthesis
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
KY386 is a DHX33 helicase inhibitor with an IC50 of 0.019 μM. KY386 inhibits the cell viability of various cancer cells. KY386 induces ferroptosis in cancer cells, and induces apoptosis in some cancer cell lines. KY386 increases the intracellular levels of ROS, LPO and Fe 2+, and decreases the level of GSH in cancer cells . KY386 inhibits the growth of gastric cancer and colon cancer xenografts in nude mice. KY386 is applicable to the related research on liver cancer, lung cancer, pancreatic cancer, colorectal cancer, gastric cancer, breast cancer, leukemia, renal cancer, prostate cancer, esophageal cancer, cervical cancer, brain cancer (glioblastoma) and melanoma .
|
-
- HY-148819A
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma .
|
-
- HY-180419
-
|
|
ERK
Apoptosis
c-Myc
|
Inflammation/Immunology
Cancer
|
|
SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup .
|
-
- HY-P991896
-
|
AT14-012
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-B0150G
-
|
Niacinamide; Nicotinic acid amide
|
Fluorescent Dye
|
|
Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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-D3141
-
|
|
Fluorescent Dye
|
|
DR probe is a "dual-key-and-lock" fluorescent probe designed based on the Resorufin (HY-123533) scaffold (Ex/Em = 647 nm/663-738 nm). DR probe can be sequentially activated by hydrogen peroxide to form the intermediate SR, which acts as a tyrosinase substrate to trigger a fluorescence turn-on signal. DR probe can distinguish normal melanocytes from melanoma cells. DR probe supports cell imaging and can be applied to mouse melanoma models to achieve melanoma diagnosis with higher accuracy and lower false-positive rates. DR probe is applicable to relevant research on melanoma .
|
-
- HY-D3140
-
|
|
Fluorescent Dye
|
|
MB-m-borate is a double-locked near-infrared fluorescence-activated probe (Ex/Em ≈ 647 nm/684 nm). MB-m-borate undergoes cascade activation by hydrogen peroxide and tyrosinase to release the fluorophore methylene blue, thereby generating a fluorescence activation response. MB-m-borate enables precise detection of melanoma in melanoma cells and mouse models. MB-m-borate can be used for melanoma research .
|
| Cat. No. |
Product Name |
Type |
-
- HY-B0150G
-
|
Niacinamide; Nicotinic acid amide
|
Biochemical Assay Reagents
|
|
Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99115
-
|
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 .
|
-
(5)
-
- HY-P991896
-
|
AT14-012
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B0150
-
-
-
- HY-N0201
-
-
-
- HY-N0202
-
-
-
- HY-122506
-
-
-
- HY-N10335
-
-
-
- HY-N6843
-
-
-
- HY-Y1177
-
-
-
- HY-B0150A
-
-
-
- HY-N3838
-
-
-
- HY-120607
-
-
-
- HY-N7484
-
-
-
- HY-117872
-
|
20-O-Acetylsartorypyrone D
|
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
Fungal
|
|
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
|
-
-
- HY-N12834
-
|
|
Apocynaceae
Structural Classification
Plants
Urceola rosea (Hook. & Arn.) D. J. Middleton
Steroids
Source Classification
|
Others
|
|
Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
|
-
-
- HY-N0201R
-
-
-
- HY-N13739
-
|
|
Terpenoids
Sesquiterpenes
Asteraceae
Taraxacum coreanum Nakai
Plants
Source Classification
|
Tyrosinase
|
|
Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
|
-
-
- HY-138098
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-126214S
-
|
|
|
JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-101460
-
|
|
|
Tetrazine
|
|
Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .
|
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0150G
-
|
Niacinamide; Nicotinic acid amide
|
Endogenous Metabolite
Sirtuin
HBV
|
Infection
Cancer
|
|
Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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 .
|
-
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: