Search Result
Results for "
G2 phase
" in MedChemExpress (MCE) Product Catalog:
9
Biochemical Assay Reagents
10
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N1428
-
-
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- HY-13442A
-
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B1939 mesylate; E7389 mesylate; ER-086526 mesylate
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Microtubule/Tubulin
Apoptosis
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Cancer
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Eribulin mesylate is an inhibitor for microtubule. Eribulin mesylate inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate exhibits antitumor efficacy in mouse model .
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-
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- HY-N6722
-
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Tridolgosir
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Apoptosis
Antibiotic
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Infection
Cancer
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Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity .
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-
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- HY-10222
-
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BMS-247550; Aza-epothilone B
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Microtubule/Tubulin
Apoptosis
Bacterial
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Cancer
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Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
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-
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- HY-N0421
-
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Cinobufagine
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Apoptosis
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Neurological Disease
Cancer
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Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
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-
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- HY-N1428A
-
-
-
- HY-157913
-
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Pyruvate Kinase
Apoptosis
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Cancer
|
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PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer .
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-
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- HY-105930
-
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D-19466
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Apoptosis
Caspase
Bcl-2 Family
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Cancer
|
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Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer .
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- HY-147895
-
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Histone Acetyltransferase
Apoptosis
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Cancer
|
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PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase .
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- HY-104013
-
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CDK
Apoptosis
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Cancer
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Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
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- HY-112607
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis .
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-
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- HY-122496
-
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Syringidin
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Apoptosis
|
Cancer
|
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Malvidin (chloride) is a bioactive compound isolated from grape. Malvidin shows cytotoxicity through the arrest of the G2/M phase of cell cycle and induction of apoptosis. Malvidin can be used for the research of cancer .
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- HY-149530
-
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EGFR
Apoptosis
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Cancer
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EGFR-IN-86 (compound 4i) is an EGFR inhibitor (IC50: 1.5 nM) with high activity against glioblastoma. EGFR-IN-86 induces apoptosis and arrests the U87 cell cycle in the G2/M phase .
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- HY-155439
-
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FAK
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Cancer
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FAK-IN-14 (compound 8d) is a focal adhesion kinase(FAK) inhibitor with an IC50 value of 0.2438 nM. FAK-IN-14 induces U87-MG cell early apoptosis and arrest the cell at the G2/M phase .
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- HY-W127705
-
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Fluorescent Dye
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Others
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Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes .
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- HY-115683
-
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Apoptosis
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Cancer
|
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NUN82647 is a potent cytotoxic compound that inhibits cell cycle at G2 phase and induces apoptosis. NUN82647 can be used for the study of leukemia .
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- HY-162276
-
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Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
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Cancer
|
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Anticancer agent 188 (compound D43) inhibits DNA synthesis in TNBC cells, leading to cell cycle arrest at the G2/M phase. Anticancer agent 188 has anti-cancer viability by inducing ROS-mediated apoptosis and DNA damage .
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- HY-124588
-
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DNA Methyltransferase
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Cancer
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MC3343, a DNMT inhibitor (EC50 of 5.7 μM) and a strong DNA binder, affects tumor proliferation by blocking OS cells in G1 or G2/M phases and induces osteoblastic differentiation through the specific re-expression of genes regulating this physiological process .
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- HY-146818
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-12 is a tubulin polymerization inhibitor (IC50=0.75 μM). Tubulin polymerization-IN-12 arrests cell cycle at G2/M phase, and exhibits cytotoxicity against cancer cells .
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- HY-149249
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Microtubule/Tubulin
Apoptosis
Histone Demethylase
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Cancer
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MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research .
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- HY-16375
-
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D-63153
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GnRH Receptor
Apoptosis
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Cancer
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Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer .
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- HY-125132
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(-)-Agelastatin A; AglA
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Apoptosis
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Cancer
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Agelastatin A ((-)-Agelastatin A; AglA), a tetracyclic alkaloid isolated from the sponge Agelas dendromorpha, induces apoptosis and arrests cells in the G2/M phase of the cell cycle, exhibiting antitumor activity .
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- HY-123369
-
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CDK
Apoptosis
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Cancer
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BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with IC50 of 2.3 nM. BMI-1026 induces apoptosis by arresting the G2-M phase .
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- HY-147896
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-29 (compound 6g) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-29 exhibits potent antiproliferative activity. Tubulin polymerization-IN-29 can induce HeLa cells arrest in G2/M phase .
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- HY-N9968
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Akt
Apoptosis
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Cancer
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Cucurbitacin C is a triterpenoid calabinoid that can be isolated from Cucurbitaceae plants. Cucurbitacin C has anti-cancer activity in vivo and in vitro. Cucurbitacin C can induce cell cycle arrest in G1 or G2/M phase and apoptosis by inhibiting Akt signaling .
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- HY-161141
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c-Met/HGFR
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Cancer
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EGFR/ C-Met-in-2 (Compound H-22) is a dual inhibitor of EGFR/c-Met. EGFR/c-Met-IN-2 inhibits cell proliferation by arresting G2/M phase. EGFR/c-Met-IN-2 has antitumor activity .
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- HY-15882
-
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Endogenous Metabolite
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Cancer
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GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
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- HY-18626
-
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Topoisomerase
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Cancer
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NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM .
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- HY-137005
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Topoisomerase
Apoptosis
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Cancer
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CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis .
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- HY-126566
-
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Fungal
HDAC
Apoptosis
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Infection
Cancer
|
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Trichostatin C is an inhibitor for histone deacetylase (HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
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- HY-156916
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-
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- HY-133838
-
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BM41440
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Parasite
PKC
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Infection
Cancer
|
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Ilmofosine (BM41440) is a potent and selective protein kinase C inhibitor. Ilmofosine induces cell cycle arrest at the G2 phase. Ilmofosine also is an anti-leishmanial agent .
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- HY-149630
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VEGFR
HDAC
Apoptosis
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Cancer
|
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VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC50s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect .
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- HY-146316
-
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Topoisomerase
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Cancer
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Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases .
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- HY-151155
-
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
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- HY-156183
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MDM-2/p53
ERK
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Cancer
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Antiproliferative agent-37 (compound 10J) shows anti-proliferative effect by arresting the cells at the G2/M phase of the cell cycle .
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- HY-138819
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Apoptosis
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Cancer
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IMB5046 is a microtubule inhibitor that induces apoptosis by blocking the G2/M phase of the cell cycle. IMB5046 has anti-tumor activity .
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- HY-146189
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Topoisomerase
Apoptosis
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Cancer
|
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Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC50 of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC50 of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells .
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- HY-N10670
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Methylpluviatolide
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Apoptosis
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Cancer
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Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity .
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- HY-N14881
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Bacterial
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Infection
Cancer
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Monorden E has the effect of arresting the cell cycle of Jurket cells in G1 and G2/M phases. Monorden E has anti-Aspergillus niger activity .
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- HY-N14866
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Bacterial
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Infection
Cancer
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Monorden B has the effect of arresting the cell cycle of Jurket cells in G1 and G2/M phases. Monorden B has anti-Aspergillus niger activity .
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- HY-N10798
-
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(-)-Kusunokinin
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Apoptosis
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Cancer
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Kusunokinin ((-)-Kusunokinin) is a nature product that could be isolated form P. nigrum. Kusunokinin has anticancer activity. Kusunokinin arrests cell cycle at G2/M phase and induce apoptosis .
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- HY-172940
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Apoptosis
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Cancer
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TBP-134 induce apoptosis primarily through DR5 and causes G2/M phase arrest. TBP-134 can be used in the research for pancreatic tumor .
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- HY-163444
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Apoptosis
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Cancer
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Apoptosis inducer 15 (Compound 3) induces cell apoptosis and cell cycle arrest at G2/M phase. Apoptosis inducer 15 is cytotoxicitic without causing DNA fragmentation .
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- HY-162108
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Apoptosis
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Cancer
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Antitumor agent-128 (compound 1a) is an antitumor agent that elicits cell cycle arrest in both the G2/M and S phases, triggering apoptosis in A549 cells .
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-
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- HY-147824
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Tubulin polymerization-IN-22 is a tubulin polymerization inhibitor with an IC50 of 8.1 μM. Tubulin polymerization-IN-22 arrests cell cycle at G2/M phase and induces apoptosis .
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-
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- HY-147848
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-27 (compound 5j) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-27 can arrest cell cycle at G2/M phase and induce apoptosis .
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-
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- HY-N10394
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Others
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Cancer
|
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Metachromins X is a sesquiterpene quinone that arrests the cell cycle progression of HeLa/Fucci2 cells at S/G2/M phase .
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- HY-164374
-
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PAK
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Cancer
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AK963/40708899 is a potent PAK1 inhibitor. AK963/40708899 suppresses the proliferation of human gastric cancer cells by downregulation of PAK1-NF-κB-cyclinB1 pathway. AK963/40708899 induces cell cycle arrest at G2 phase and reduces the migration and invasion. AK963/40708899 inhibits the formation of filopodia and promots cell adhesion which in turn inhibits invasive potential of gastric cells by negatively regulating PAK1-LIMKl-cofilin and PAK1-ERK-FAK pathways .
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- HY-122151
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
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MPT0B002 is a potent microtubule inhibitor with anticancer activities. MPT0B002 disrupts tubulin polymerization, induces apoptosis, and arrests cell cycle at the G2/M phase .
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- HY-163808
-
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Apoptosis
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Cancer
|
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Anticancer agent 237 (compound 13) is a potent anticancer agent. Anticancer agent 237 shows cytotoxicity. Anticancer agent 237 induces apoptosis and cell cycle arrest at the S and G2/M phases .
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- HY-100761
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin .
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- HY-149221
-
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Apoptosis
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Cancer
|
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Apoptosis inducer 11 (compound 3u) induces apoptosis through the mitochondrial pathway. Apoptosis inducer 11 induces a block in G2/M, a strong decrease in S phase in non-Hodgkin lymphoma cell lines .
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- HY-144299
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
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Tubulin polymerization-IN-5 (compound 20q) is a potent tubulin inhibitor with potential anticancer activities. Tubulin polymerization-IN-5 can arrest ESCC cells at G2/M phase and cause cells apoptosis .
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- HY-156266
-
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Rhiz
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Others
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Cancer
|
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Rhizochalinin (Rhiz) is a cytotoxic sphingolipid. Rhizochalinin (Rhiz) counteracts glioblastoma cell proliferation by inducing apoptosis, G2/M-phase cell cycle arrest, and inhibition of autophagy. Rhizochalinin (Rhiz) can be used for human glioblastoma research .
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- HY-117473
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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DAT-230 is a microtubule inhibitor. DAT-230 induces cell apoptosis and results in microtubule de-polymerization and G2/M phase arrest. DAT-230 inhibits cell growth in vitro and in vivo .
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- HY-108053
-
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Parasite
Apoptosis
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Infection
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CDRI-97/78 is an antimalarial agent. CDRI-97/78 has phototoxicity and can induce cell apoptosis and G2/M phase arrest. CDRI-97/78 can be used for the research of infection .
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- HY-155686
-
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Microtubule/Tubulin
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Cancer
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Tubulinpolymer-in-44 (compound 7w) is a strong and effective Tubulin inhibitor, with an IC50 value of 0.21 μM. Tubulinpolymer-in-44 induces apoptosis by arresting G2/M phase, which can be used for cancer research.
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- HY-161256
-
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Tubulin inhibitor 41 (Compd D19), a promising anti-GBM (glioblastoma) lead compound and tublin inhibitor with BBB permeability, induces G2/M phase arrest, resulted in cell apoptosis and inhibits the migration of U87 cells .
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- HY-169106
-
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Topoisomerase
Apoptosis
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Cancer
|
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Topoisomerase inhibitor 4 (compound 45) is a potent Topoisomerase1/2 inhibitor. Topoisomerase inhibitor 4 causes cell cycle arrest in the G2/M phase by inducing Apoptosis. Topoisomerase inhibitor 4 has antitumor activity .
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- HY-172116
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-
- HY-152099
-
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|
Apoptosis
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Cancer
|
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Antiproliferative agent-19 (compound 4a) is an anti-cancer agent that exerts anti-proliferative effects on lung cancer cells by inducing apoptosis. antiproliferative agent-19 also induces cell cycle arrest in the G2/M phase .
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- HY-155314
-
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Microtubule/Tubulin
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Cancer
|
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Tubulin polymerization-IN-50 (compound 7n) is a inhibitor of tubulin polymerization, with the IC50 of 5.05 μM in SK-Mel-28 cells. Tubulin polymerization-IN-50 induces the cell cycle arrest in the G2/M phase .
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- HY-146188
-
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Topoisomerase
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Cancer
|
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Topoisomerase II inhibitor 8 (compound 22) is a potent topoisomerase II inhibitor, with an IC50 of 0.52 μM. Topoisomerase II inhibitor 8 exhibits good anti-proliferative activities and can arrest the cell cycle at G2/M phase .
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- HY-162291
-
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Src
Apoptosis
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Cancer
|
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Lck-IN-3 (compound 7m) is an LCK inhibitor targeting acute lymphoblastic leukemia (ALL) that inhibits LCK phosphorylation. Lck-IN-3 can induce cell cycle arrest in the G2/M phase, leading to apoptosis in ALL cells .
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- HY-144754
-
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VEGFR
Apoptosis
|
Cancer
|
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VEGFR-2-IN-13 (Compound 19a) is a potent VEGFR-2 inhibitor with an IC50 of 3.4 nM. VEGFR-2-IN-13 disrupts the HepG2 cell cycle by arresting the G2/M phase and induces apoptosis .
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- HY-172104
-
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EGFR
Apoptosis
|
Cancer
|
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EGFR-IN-143 (Compound 5f) is a potent EGFR inhibitor with an IC50 value of 0.15 μM. EGFR-IN-143 induces apoptosis by arresting the cell cycle in the G2/M phase. EGFR-IN-143 has antitumor activity .
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- HY-147783
-
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MDM-2/p53
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Cancer
|
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Anticancer agent 68 is (Compound 12) is an anti-cancer agent. Anticancer agent 68 arrests the cells at the G2/M phase and induces programmed cell death. Anticancer agent 68 induces upregulation of tumor suppression via activation of p53 & PTEN .
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- HY-143266
-
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Topoisomerase
Apoptosis
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Cancer
|
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Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
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- HY-161067
-
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EGFR
Apoptosis
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Cancer
|
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EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFR T790M .
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- HY-146711
-
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Microtubule/Tubulin
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Cancer
|
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Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity .
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- HY-161358
-
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FAK
Apoptosis
|
Cancer
|
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FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS .
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- HY-144340
-
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DNA/RNA Synthesis
Apoptosis
|
Cancer
|
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Antitumor agent-43 (Compound 4B) is a potent antitumor agent, with an IC50of 0.5 µM for (T-24 cell). Antitumor agent-43 (Compound 4B) induces cell cycle arrest at G2/M phase .
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- HY-106176
-
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Microtubule/Tubulin
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Cancer
|
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BMS-184476 is a selective microtubule inhibitor with potent antitumor activity. BMS-184476 induces G2/M phase arrest and promotes tumor cell apoptosis. BMS-184476 is promising for research of solid tumors, such as non-small cell lung cancer .
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- HY-122496R
-
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Syringidin (Standard)
|
Reference Standards
Apoptosis
|
Cancer
|
|
Malvidin (chloride) (Standard) is the analytical standard of Malvidin (chloride). This product is intended for research and analytical applications. Malvidin (chloride) is a bioactive compound isolated from grape. Malvidin shows cytotoxicity through the arrest of the G2/M phase of cell cycle and induction of apoptosis. Malvidin can be used for the research of cancer .
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- HY-161046
-
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Polo-like Kinase (PLK)
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Cancer
|
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PLK1-IN-8 (compound TE6) is a PLK1 inhibitor, and inhibits cell proliferation by blocking the cell cycle at G2 phase. PLK1-IN-8 shows anticancer activity in vivo .
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-
- HY-122249
-
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Microtubule/Tubulin
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Cancer
|
|
MT-7 is a potent mitotic inhibitor. MT-7 shows antiproliferative activity. MT-7 induces cell cycle arrest at G2/M phase. MT-7 induces specific, reversible mitotic arrest and inhibits the polymerization of cellular microtubules .
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-
- HY-W278582
-
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Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 14 is a potent topoisomerase II inhibtor. Topoisomerase II inhibitor 14 induces apoptosis and arrests cell cycle at S phase and G2-M phases. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO. Topoisomerase II inhibitor 14 can be used for the study of neck squamous cell carcinoma (HNSCC) .
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- HY-161339
-
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Apoptosis
Sirtuin
|
Cancer
|
|
SIRT2-IN-13 (compound 7c) is an inhibitor of SIRT2 and induces apoptosis. SIRT2-IN-13 selectively inhibits colon cancer and leukemia cells and arrests the cell cycle in the G2 phase .
|
-
- HY-149370
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-60 (compound 21a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-60 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis .
|
-
- HY-120027
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Kribb3 is an inhibitor for microtubule. KRIBB3 inhibits the proliferation of cancer cells with GI50 of 0.2-2.5 μM, arrests cell cycle at G2/M phase, and induces apoptosis in HCT-116. Kribb3 exhibits antitumor activity in mouse models .
|
-
- HY-149369
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-59 (compound 13a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-59 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis .
|
-
- HY-119118
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
J-30 is an orally active and potent tubulin inhibitor (IC50=15-20 nM). J-30 disrupts microtubule polymerization and induces G2/M phase arrest. J-30 is promising for research of solid tumors (e.g., gastric, oral) .
|
-
- HY-N0421R
-
|
Cinobufagine (Standard)
|
Reference Standards
Apoptosis
|
Neurological Disease
Cancer
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-13451R
-
|
|
Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
Citric acid (Standard) is the analytical standard of Citric acid. This product is intended for research and analytical applications. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice .
|
-
- HY-W747797
-
|
|
Isotope-Labeled Compounds
Apoptosis
|
Cancer
|
|
Cinobufagine-d3 is the deuterium labeled Cinobufagin (HY-N0421). Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
- HY-145438
-
|
|
Others
|
Cancer
|
|
Antitumor agent-38 is a potent antitumor agents. Antitumor agent-38 shows antiproliferative activity for cancer cells. Antitumor agent-38 induces cell cycle arrest at the late S and G2/M phase without interfering with microtubule formation or cell morphology[1].
|
-
- HY-149252
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 32 shows anti-proliferative activity and inhibits microtubule polymerization. Tubulin inhibitor 32 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin inhibitor 32 shows anti-tumor activity .
|
-
- HY-114545
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
5HPP-33 is an inhibitor for tubulin polymerization with IC50 of 8.1 μM. 5HPP-33 inhibits the proliferation of leukemia cell and multiple myeloma cells with IC50 of 1-10 μM, arrests the cell cycle at G2/M phase, and induces apoptosis .
|
-
- HY-162311
-
|
|
Ferroptosis
Autophagy
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Anticancer agent 194 (compound 10p) is a ferroptosis and autophagy inducer. Anticancer agent 194 arrests colon cancer cell cycle at G2/M phase, but can't induce cell apoptosis. Anticancer agent 194 independently triggeres cell ferroptosis and autophagy through the massive accumulation of ROS .
|
-
- HY-N3446
-
|
|
Apoptosis
|
Cancer
|
|
IVHD-valtrate, an active Valeriana jatamansi derivative, is against human ovarian cancer cells in vitro and in vivo. IVHD-valtrate induces cancer cells apoptosis and arrests the ovarian cancer cells in the G2/M phase. IVHD-valtrate has the potential to be a novel chemotherapeutic agent for the human ovarian cancer research .
|
-
- HY-116664
-
|
|
Apoptosis
Ras
Raf
Caspase
|
Cancer
|
|
DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer .
|
-
- HY-147771
-
|
|
CDK
Apoptosis
|
Cancer
|
|
ZLWT-37 is a potent, orally active CDKs inhibitor with IC50 values of 0.002 μM and 0.054 μM against CDK9 and CDK2, respectively. ZLWT-37 induces apoptosis and arrests the cell cycle in the G2/M phase in HCT116 cells .
|
-
- HY-N15052
-
|
|
Bacterial
|
Infection
Cancer
|
|
Monorden C has the effect of arresting the cell cycle of Jurket cells in G1 and G2/M phases. Monorden C has anti-Aspergillus niger activity .
|
-
- HY-119736
-
|
|
Others
|
Others
|
|
Leptolstatin is an inhibitor of the progression of G1 and G2 phases of the mammalian cell cycle. Leptolstatin can be extracted from the fermentation broth of Streptomyces sp. SAM1595 .
|
-
- HY-19257
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Triplatin tetranitrate is a novel trinuclear platinum complex. Triplatin tetranitrate blocks G2/M phase. Triplatin tetranitrate can covalently bind to the DNA bases. Triplatin tetranitrate exhibits significant antitumor effects against neuroblastoma .
|
-
- HY-181051
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK1-IN-16 is a selective polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.25 nM. PLK1-IN-16 exhibits lower inhibitory potency against PLK2 and PLK3, induces G2 phase cell cycle arrest, induces apoptosis, and exhibits antiproliferative activity against tumor cells. PLK1-IN-16 can be stable under simulated gastric acid environmental conditions, and acceptable CYP 450 inhibition. PLK1-IN-16 can be used for the study of triple-negative breast cancer (TNBC), breast cancer, leukemia .
|
-
- HY-181675
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma .
|
-
- HY-108869R
-
|
DPDP (Standard)
|
Reference Standards
Drug Metabolite
|
Inflammation/Immunology
|
|
Malvidin (chloride) (Standard) is the analytical standard of Malvidin (chloride). This product is intended for research and analytical applications. Malvidin (chloride) is a bioactive compound isolated from grape. Malvidin shows cytotoxicity through the arrest of the G2/M phase of cell cycle and induction of apoptosis. Malvidin can be used for the research of cancer .
|
-
- HY-N12331
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Ohchinolide B is a tubulin inhibitor. Ohchinolide B inhibits microtubule polymerization (IC50=2.3 μM) and induces G2/M phase cell cycle arrest via mitochondrial apoptotic pathways. Ohchinolide B is promising for research of solid tumors (e.g., breast, lung cancer) .
|
-
- HY-149003
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .
|
-
- HY-146409
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-59 (Compound 13b) is a potent antitumor agent. Antitumor agent-59 effectively inhibits the proliferation and migration of HCT116 cells. Antitumor agent-59 induces HCT116 cell apoptosis and arrests the cell cycle at the G2/M phase .
|
-
- HY-10222R
-
|
BMS-247550 (Standard); Aza-epothilone B (Standard)
|
Reference Standards
Microtubule/Tubulin
Apoptosis
Bacterial
|
Cancer
|
|
Ixabepilone (Standard) is the analytical standard of Ixabepilone. This product is intended for research and analytical applications. Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
|
-
- HY-146390
-
|
|
Autophagy
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antiproliferative agent-5 (compound 4o) can significantly and irreversibly inhibit proliferation of gastric cancer cells. Antiproliferative agent-5 causes the G2/M phase arrest, and induces ROS accumulation and activation of autophagy. Antiproliferative agent-5 can be used for researching anticancer .
|
-
- HY-144394
-
|
|
Apoptosis
c-Met/HGFR
|
Cancer
|
|
Antitumor agent-45 (Compound 21) could induce and stimulate A549 cells apoptosis in G0/G1 and G2/M phase. Antitumor agent-45 (Compound 21) inhibits c-Met expression to regulate the growth of tumor cells .
|
-
- HY-146093
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase .
|
-
- HY-172595
-
|
|
Apoptosis
E1/E2/E3 Enzyme
|
Cancer
|
|
Apoptosis inducer 48 (5d) is an apoptotic agent. Apoptosis inducer 48 inhibits the growth of triple-negative breast cancer cells. Apoptosis inducer 48 attenuates proteasomal degradation via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic .
|
-
- HY-148265
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antiproliferative agent-14 (compound 3b) a potent tubulin polymerization inhibitor, with an IC50 of 3.41 μM. Antiproliferative agent-14 has excellent antiproliferative activity. Antiproliferative agent-14 possess the ability to arrest cells at G2/M phases of the cell cycle .
|
-
- HY-W009156
-
-
- HY-B2201
-
-
- HY-101990
-
|
|
VEGFR
|
Others
|
|
IMS2186 is an anti-choroidal neovascularization (CNV) agent that inhibits angiogenesis upstream of VEGF. IMS2186 can arrest cancer cell cycle in G2/M phase, thus exerting anti-proliferation and anti-angiogenesis effects. IMS2186 has no intraocular toxicity and reduces the amount of eye leakage and diseased cells .
|
-
- HY-158233
-
|
|
Apoptosis
VEGFR
|
Cancer
|
|
Apoptotic agent-4 (Compound 9) is a apoptosis inducer. Apoptotic agent-4 inhibits VEGFR-2 with an IC50 of 0.5717 μM. Apoptotic agent-4 inhibits cancer cell proliferation and arrests the cell at both the G2/M and Pre-G1 phases .
|
-
- HY-163523
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PYRIB-SO 2 is a potent antimitotic agent. PYRIB-SO 2 shows antiproliferative activity and induces cell cycle arrest at G2/M phase. PYRIB-SO 2 reduces and disruptes microtubule structures. PYRIB-SO 2 binds to the colchicine-binding site (C-BS) of α, β-tubulin .
|
-
- HY-118798
-
|
NSC663285
|
Phosphatase
|
Cancer
|
|
DA 3003-2 is a potent and selectively Cdc25 inhibitor. DA 3003-2 shows antiproliferative activity. DA 3003-2 induces cell cycle arrest at the G2/M phase and increases the expression of P-tyr 15 Cdc2. DA 3003-2 has the potential for the research of prostate cancer .
|
-
- HY-149363
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-43 (compound 15h) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-43 disrupts cellular microtubule networks by targeting the Colchicine (HY-16569) site, and promots cell cycle arrest of leukemia cells at G2/M phase and cell apoptosis, as well as inhibiting angiogenesis .
|
-
- HY-161268
-
-
- HY-100789
-
|
|
Apoptosis
Polo-like Kinase (PLK)
Mitosis
|
Cancer
|
|
ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 μM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity .
|
-
- HY-150004
-
|
|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-3 (Compound 15f) is a dual c-Met and HDAC inhibitor with IC50 values of 12.50 nM and 26.97 nM against c-Met and HDAC1, respectively. c-Met/HDAC-IN-3 induces apoptosis and cause cell cycle arrest in G2/M phase .
|
-
- HY-N0047
-
|
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
|
-
- HY-143272
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase .
|
-
- HY-175853
-
|
|
Topoisomerase
Apoptosis
Caspase
|
Cancer
|
|
Topoisomerase II-IN-24 is a Topoisomerase IIα inhibitor with an IC50 of 41.67 μM. Topoisomerase II-IN-24 can inhibit cancer cells proliferation, induce G2/M phase arrest and induce apoptosis. Topoisomerase II-IN-24 can be used for the research of cancer, such as colon cancer .
|
-
- HY-N2374R
-
|
|
Reference Standards
Apoptosis
|
Cancer
|
|
Eupatorin (Standard) is the analytical standard of Eupatorin. This product is intended for research and analytical applications. Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage .
|
-
- HY-163740
-
|
|
Apoptosis
Necroptosis
VEGFR
|
Cancer
|
|
VEGFR-2-IN-46 (compound 4d) is a potent VEGFR-2 inhibitor with an EC50 value of 67.0 nM. VEGFR-2-IN-46 shows cytotoxicity and induces cell cycle arrest at the G2/M phase. VEGFR-2-IN-46 induces necrosis and apoptosis .
|
-
- HY-W008606
-
-
- HY-147906
-
|
|
Apoptosis
PARP
|
Cancer
|
|
Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity .
|
-
- HY-118713
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Kuanoniamine A is a pyridoacridine alkaloid and also an anticancer agent. Kuanoniamine A inhibits DNA synthesis, induces apoptosis, and regulates the cell cycle by reducing the proportion of cells in the G2/M phase. Kuanoniamine A inhibits the proliferation of human lymphocytes. Kuanoniamine A can be used in research related to breast cancer, glioma, non-small cell lung cancer, and melanoma .
|
-
- HY-N10018
-
|
25-Anhydrocimigenol xyloside
|
Caspase
|
Cancer
|
|
Cimiside E (25-Anhydrocimigenol xyloside) is a triterpene xyloside, Cimiside E possesses apoptotic action on gastric cancer cells, with an IC50 value of 14.58 μM. Cimiside E induces cell cycle arrest at G2/M phase, and mediates apoptosis through the induction of the caspase cascade for both the extrinsic and intrinsic pathways .
|
-
- HY-151985
-
|
|
Apoptosis
|
Cancer
|
|
TACC3 inhibitor 1 is a potent and cross the blood-brain barrier TACC3 inhibitor. TACC3 inhibitor 1 induces Apoptosis and cell cycle arrest at G2/M phase. TACC3 inhibitor 1 induces the generation of intracellular ROS. TACC3 inhibitor 1 shows antiproliferative and anti-tumor activity .
|
-
- HY-170563
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-72 (Compound 4a4) is an anticancer agent that acts as a tubulin polymerization inhibitor. It inhibits tubulin polymerization by binding to the colchicine site, leading to cancer cell arrest in the G2/M phase and inducing their apoptosis (Apoptosis). Tubulin polymerization-IN-72 has an IC50 of 0.4-2.7 nM against cancer cells.
|
-
- HY-12300A
-
|
CFI-400945 hydrochloride
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model .
|
-
- HY-147892
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-143265
-
|
|
Topoisomerase
Apoptosis
Caspase
|
Cancer
|
|
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect .
|
-
- HY-149889
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFR C797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
|
-
- HY-126246
-
|
|
Phosphatase
|
Cancer
|
|
CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase .
|
-
- HY-146666
-
|
|
Apoptosis
STAT
|
Cancer
|
|
STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-173613
-
|
|
Ferroptosis
|
Cancer
|
|
VEGFR-2-IN-68 (13b) is a VEGFR-2 inhibitor, with an IC50 of 41.51 nM. VEGFR-2-IN-68 (13b) induces apoptosis and G2/M phase arrest. VEGFR-2-IN-68 (13b) exhibits anti-metastatic properties in cancer cells .
|
-
- HY-146718
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities .
|
-
- HY-B1357
-
-
- HY-146407
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity .
|
-
- HY-B1295
-
|
Litarex tetrahydrate
|
Apoptosis
Endogenous Metabolite
Bacterial
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Lithium citrate (Litarex) tetrahydrate is a natural preservative and food tartness enhancer. Lithium citrate tetrahydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Lithium citrate tetrahydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Lithium citrate tetrahydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-144797
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 22 (compound 4c) is a potent inhibitor of tubulin with anti-angiogenesis and anti-cancer properties. Tubulin inhibitor 22 arrests MGC-803 cell cycle at G2/M phase. Tubulin inhibitor 22 dose-dependently causes Caspase-induced apoptosis of MGC-803 cells through mitochondrial dysfunction .
|
-
- HY-161970
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis .
|
-
- HY-161151
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor . Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells .
|
-
- HY-101989
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-24 (compound HMBA) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-24 inhibits MCF-7 cells proliferation. Tubulin polymerization-IN-24 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-24 increase the GTP hydrolysis rate and inhibits microtubule assembly .
|
-
- HY-146136
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFR T790M and EGFR T790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis .
|
-
- HY-163924
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 25 (Compound 4H) inhibits the proliferation of cell BGC-823 with IC50 of 0.37 μM. Apoptosis inducer 25 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 25 exhibits good pharmacokinetic properties in rats .
|
-
- HY-162360
-
|
|
Apoptosis
EGFR
Caspase
Bcl-2 Family
|
Cancer
|
|
EGFR-IN-109 (compound 4) is an EGFR inhibitor, with the IC50 values of 25.8 and 182.3 nM for EGFR WT and EGFR T790M, respectively. EGFR-IN-109 arrests the cancer cells’ growth at the G2/M phase and induces both early and late apoptosis. EGFR-IN-109 can be used in cancer research .
|
-
- HY-183271
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin-IN-67 is a tubulin inhibitor. Tubulin-IN-67 binds to the colchicine-binding site of tubulin, inhibiting tubulin polymerization. Tubulin-IN-67 arrests cancer cell cycle at the G2/M phase and triggers apoptosis in cancer cells. Tubulin-IN-67 can be used for the research of hepatocellular carcinoma, cervical carcinoma, breast carcinoma .
|
-
- HY-150592
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-2 (compound 12Aj) is a potent Aurora kinase inhibitor with IC50 values of 90 and 152 nM for Aurora A and Aurora B. Aurora kinase-IN-2 arrests cell cycle at G2/M phase by regulating cyclin B1 and cdc2. Aurora kinase-IN-2 can be used for cancer research .
|
-
- HY-182031
-
|
|
EGFR
Apoptosis
Bcl-2 Family
Survivin
|
Cancer
|
|
JS04 is a EGFR L858R/T790M kinase inhibitor. JS04 activates both endogenous and exogenous apoptosis (apoptosis) pathways and induces G2/M phase arrest of the cell cycle. JS04 is applicable to the research of drug-resistant non-small cell lung cancer .
|
-
- HY-173406
-
|
|
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
|
RSK-IN-2 (Compound 3e) is a RSK inhibitor, with IC50 s of 37.89 nM (RSK2), 30.78 nM (RSK1), 20.51 nM (RSK3), 91.28 nM (RSK4). RSK-IN-2 inhibits tumor cell proliferation, induces apoptosis and causes cell cycle arrest in the G2/M phase .
|
-
- HY-162227
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
|
-
- HY-147901
-
|
|
Histone Demethylase
CDK
Apoptosis
Caspase
|
Cancer
|
|
KDM1/CDK1-IN-1 (compound 4) is a potent KDM1 and CDK1 inhibitor, with IC50 values of 0.096 and 0.078 μM, respectively.KDM1/CDK1-IN-1 induces cell cycle arrest at G2/M phase and apoptosis in HOP-92 cells. KDM1/CDK1-IN-1 exhibits potent cytotoxic activity against the CCRF-CEM, HOP-92 and Hep-G2 cells, with IC50 values of 16.34, 3.45 and 7.79 μM, respectively .
|
-
- HY-179696
-
|
|
Microtubule/Tubulin
Drug Derivative
|
Cancer
|
|
destabilizing agent-3 (HY-179695). Microtubule destabilizing agent-3 is a microtubule destabilizing agent. Microtubule destabilizing agent-3 exerts its antimyeloma phenotypes by destabilizing microtubules and promoting mitotic arrest, leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis .
|
-
- HY-161338
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-61 (Compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-61 destroys the microtubule skeleton, blocks the cell cycle in G2/M phase, induces Apoptosis, and inhibits cancer cell migration and colony formation. Tubulin polymerization-IN-61 shows antitumor activity in vivo against 4T1 xenograft model .
|
-
- HY-177501
-
|
|
CDK
Apoptosis
|
Cancer
|
|
Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer .
|
-
- HY-147854
-
|
|
Raf
Apoptosis
|
Cancer
|
|
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM .
|
-
- HY-170778
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-77 (Compound 15c) is a tubulin polymerization inhibitor that exerts anti-glioblastoma activity by inhibiting tubulin polymerization. Tubulin polymerization-IN-77 demonstrates significant blood-brain barrier permeability, effectively inducing G2/M phase arrest and triggering apoptosis in GBM cells, while also significantly inhibiting tumor cell migration .
|
-
- HY-144811
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK2-IN-9 is a potent CDK2 inhibitor with an IC50 of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma .
|
-
- HY-155541
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-110 (compound 13) is an anticancer imidazotetrazine with good permeability properties. Antitumor agent-110 arrests cell cycel at G2/M phase, and induces apoptosis . Antitumor agent-110 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-147786
-
|
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-5 (Compound 4b) is a potent inhibitor of TGFβRI with an IC50 of 0.08 μM. TGFβRI-IN-5 displays amazing anticancer activity 5–7 times that of reference agent against all the tested cell lines. TGFβRI-IN-5 enhances apoptosis and arrested G2/M phase of cell cycle .
|
-
- HY-103257
-
|
NSC656158
|
Microtubule/Tubulin
|
Cancer
|
|
CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity .
|
-
- HY-118976
-
|
CGP-74514A
|
CDK
Apoptosis
|
Cancer
|
|
CGP-74514 hydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50: 25 nM). CGP-74514 hydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 hydrochloride is promising for research of bladder cancer .
|
-
- HY-114413
-
|
|
HSP
Apoptosis
|
Cancer
|
|
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration .
|
-
- HY-N4164
-
|
|
Fungal
Apoptosis
|
Infection
Cancer
|
|
Schinifoline is a 4-quinolinone found in Zanthoxylum schinifolium. Schinifoline can inhibit cancer cells proliferation, cause G2/M phase arrest and induce apoptosis. Schinifoline can improve radiosensitizing effect of cancer cells. Schinifoline shows anti-fungal activity. Schinifoline can be used for the researches of cancer and infection, such as lung cancer and C. albicans infection .
|
-
- HY-171183
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
AB8939 is an effective small moleculeMicrotubule/Tubulin polymerization inhibitor with anti-tumor activity (it inhibits tumor cell proliferation with an IC50 of less than 10 nM). AB8939 can effectively evade resistance mechanisms mediated by things like P-glycoprotein and myeloperoxidase. AB8939 can induce G2/M phase cell cycle arrest and apoptosis in cells .
|
-
- HY-156285
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase .
|
-
- HY-144786
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer .
|
-
- HY-172401
-
|
|
APC
Apoptosis
|
Cancer
|
|
CDC20-IN-2 (14c), a Cdc20 inhibitor (KD: 7.65 μM), causes G2/M phase arrest and promotes DNA damage accumulation. CDC20-IN-2 (14c) stabilizes key substrates such as Cyclin B1 and Bim, leading to enhanced apoptosis and suppression of tumor cell proliferation and migration .
|
-
- HY-N9942
-
|
|
Apoptosis
Autophagy
NF-κB
p38 MAPK
PI3K
Akt
mTOR
STAT
JAK
|
Inflammation/Immunology
Cancer
|
|
Physalin A is a biologically active withanolide. Physalin A shows anti-inflammatory, antifibrotic and ameliorative effects on autophagy in models of disc degeneration. Physalin A has antitumor activity and can induce apoptosis, ROS production and G2/M phase cell cycle arrest. Besides. Physalin A can significantly increase the activity of quinone reductase and increase the expression of detoxifying enzymesc .
|
-
- HY-144766
-
|
|
Apoptosis
|
Cancer
|
|
ATX inhibitor 13 (10c) is an orally active and potent ATX inhibitor, with an IC50 of 3.4 nM. ATX inhibitor 13 inhibits proliferation and migration, and induces apoptosis and G2 phase arrest in RAW264.7 cells. ATX inhibitor 13 suppresses tumor cell colony formation .
|
-
- HY-N1428S2
-
-
- HY-N1428S3
-
-
- HY-N1428S
-
-
- HY-N1428R
-
-
- HY-N1428S1
-
-
- HY-N1428S6
-
-
- HY-N1428AR
-
|
|
Reference Standards
Endogenous Metabolite
Apoptosis
Bacterial
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid monohydrate (Standard) is the analytical standard of Citric acid monohydrate (HY-N1428A). This product is intended for research and analytical applications. Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-162580
-
|
|
SphK
|
Cancer
|
|
SphK2-IN-3 (compound 12q) is a selective active sphingosine kinase-2 inhibitor. SphK2-IN-3 has anti-proliferative activity against various cancer cells, inducing G2 phase arrest and apoptosis in liver cancer cells HepG2 .
|
-
- HY-149800
-
|
|
PARP
Apoptosis
Caspase
|
Cancer
|
|
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer .
|
-
- HY-182035
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC8-IN-16 is a selective histone deacetylase 8 (HDAC8) inhibitor with an IC50 of 0.16 μM. HDAC8-IN-16 induces cell apoptosis, triggers G2/M phase cell cycle arrest, and moderately inhibits cancer cell proliferation. HDAC8-IN-16 is applicable to relevant research on colorectal cancer .
|
-
- HY-149291
-
|
|
ATM/ATR
Apoptosis
|
Cancer
|
|
ATM Inhibitor-7 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. ATM Inhibitor-7 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). ATM Inhibitor-7 combines with CPT-11 shows antitumor activity .
|
-
- HY-15149
-
|
FK 228; FR 901228; NSC 630176
|
HDAC
Apoptosis
|
Cancer
|
|
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
|
-
- HY-182039
-
|
|
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-89 is a tubulin polymerization inhibitor. Tubulin polymerization-IN-89 binds to the colchicine-binding site on tubulin heterodimers, disrupting tubulin polymerization and microtubule formation. Tubulin polymerization-IN-89 induces apoptosis in melanoma cells and arrests the cell cycle at the G2/M phase. Tubulin polymerization-IN-89 can be used in studies related to metastatic melanoma .
|
-
- HY-143447
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-8 concentration-dependently causes cell cycle arrest at the G2/M phase in HCT116 tumor cells, and displays a significant inhibition of tubulin polymerization with an IC50 value of 12.7 μM. Tubulin polymerization-IN-8 has the potential for the research of cancer diseases [ 1].
|
-
- HY-146021
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .
|
-
- HY-183790
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
|
Cancer
|
|
SMU-G4 is a Tubulin polymerization inhibitor. SMU-G4 induces G2/M phase cell cycle arrest, triggers Apoptosis, and upregulates the expression of Cleaved-Caspase 3. SMU-G4 exhibits in vivo anti-tumor activity in melanoma xenograft models. SMU-G4 can be used for research related to melanoma .
|
-
- HY-130558
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
SL-1-73 is a tubulin ligand. SL-1-73 exhibits antitumor activity against esophageal squamous cell carcinoma (ESCC) both in vitro and in vivo by inhibiting microtubule assembly, inducing G2/M phase cell cycle arrest and apoptosis, and disrupting tumor blood vessels. SL-1-73 can be used for the research of ESCC and other tumors .
|
-
- HY-146743
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors .
|
-
- HY-148592
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
|
-
- HY-160853
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 42 (Compound 14b) dose-dependently inhibited the activity of β-microtubulin (IC50 = 3.5 µM).Tubulin inhibitor 42 interferes with microtubule dynamic homeostasis, resulting in the arrest of the cancer cell cycle in the G2/M phase and inducing apoptosis. Tubulin inhibitor 42 significantly inhibits the angiogenic process in vitro and in vivo, preventing vascularization and tumor growth .
|
-
- HY-120490
-
|
|
Apoptosis
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
NMK-TD-100 is a modulator for microtubule. NMK-TD-100 binds to tubulin, inhibits the tubulin polymerization with an IC50 of 17.5 µM, inhibits mitosis, and decreases mitochondrial membrane potential (MMP). NMK-TD-100 inhibits the proliferation of HeLa with an IC50 of 1.42 µM, arrests cell cycle at G2/M phase, induces apoptosis in HeLa .
|
-
- HY-104013R
-
|
|
Reference Standards
CDK
Apoptosis
|
Cancer
|
|
Aminopurvalanol A (Standard) is the analytical standard of Aminopurvalanol A (HY-104013). This product is intended for research and analytical applications. Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
|
-
- HY-161617
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
LASSBio-2052 is a derivative of N-acylhydrazone with antitumor activity against hepatocellular carcinoma (HCC). LASSBio-2052 inhibits HCC cells HepG2 and Hep3B, with IC50 of 18 and 41 μM. LASSBio-2052 arrests the cell cycle at G2/M phase, through downregulation of FOXM1. LASSBio-2052 induces apoptosis in HCC cells .
|
-
- HY-155841
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
|
-
- HY-110359
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CGP-74514 dihydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 dihydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 dihydrochloride is promising for research of bladder cancer .
|
-
- HY-150765
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .
|
-
- HY-161153
-
|
|
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 9 (Compound O-7) is a 2-Aryl-1H-benzo [d] imidazole derivative with in vitro anticancer activity. Microtubule inhibitor 9 can induce cell cycle arrest at the G2/M phase and early apoptosis. Microtubule inhibitor 9 inhibits cancer cell migration by inhibiting wound healing and colony formation .
|
-
- HY-169882
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 49 (Compound 18) is an inhibitor for tubulin polymerization with an IC50 of 48 μM. Tubulin inhibitor 49 disrupts the cell microtubule network, arrests the cell cycle at G2 phase, and exhibits cytotoxicity (IC50=8.8 μM in HeLa cell). Tubulin inhibitor 49 can be used in the research of cervical cancer .
|
-
- HY-155781
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-N1428CA
-
|
|
Apoptosis
Endogenous Metabolite
Bacterial
|
Cardiovascular Disease
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Ferric citrate, suitable for cell culture is a natural preservative and food tartness enhancer. Ferric citrate, suitable for cell culture induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Ferric citrate, suitable for cell culture causes oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Ferric citrate, suitable for cell culture is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-W127841
-
-
- HY-129356
-
|
|
Antibiotic
ADC Payload
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Seco-Duocarmycin SA is a DNA alkylator. Seco-Duocarmycin SA is an antitumor antibiotic (IC50 = 10 pM). Seco-Duocarmycin SA can induce a concentration-dependent increase in apoptotic cell death. Seco-Duocarmycin SA can lead to significant cell cycle arrest in S and G2/M phases. Seco-Duocarmycin SA acts as an ADC cytotoxin for antibody-drug conjugates .
|
-
- HY-P99662
-
|
MLN0264; TAK-264
|
Antibody-Drug Conjugates (ADCs)
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
Indusatumab vedotin (MLN-0264; AKT-264) is an antibody-drug conjugate (ADC) consisting of the human anti-guanylate cyclase C (GCC) antibody linked to a microtubule-disruptor Monomethyl auristatin (HY-15162). Indusatumab vedotin has anti-proliferative effects on pancreas cancer cell lines. Indusatumab vedotin arrests cell cycle at G2/M phase, and induces apoptosis .
|
-
- HY-149376
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM，24 h) mediates mitotic arrest，blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa，MCF7，and U87 MG cells .
|
-
- HY-121214R
-
-
- HY-115565
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CGP-74514 (Compound 13) is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC50=25 nM). CGP-74514 inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G2/M phase and induces tumor cell apoptosis. CGP-74514 is promising for research of bladder cancer .
|
-
- HY-156737
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-49 (compound 12d) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-49 bound to colchicine site on tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-49 induces cell cycle arrest at G2/M phase and apoptosis. Tubulin polymerization-IN-49 has anticancer active and prevents tumor generation, inhibits tumor proliferation and angiogenesis .
|
-
- HY-163923
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with IC50 of 1.2-4.8 μM. Apoptosis inducer 24 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 24 exhibits antitumor efficacy in mice, without significant toxicity (LD50 is 91.2 mg/kg) .
|
-
- HY-176738
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antitumor agent-204 (compound 15a) is a potent antitumor agent. Antitumor agent-204 shows cytotoxicity. Antitumor agent-204 induces nitric oxide (NO) release and reactive oxygen species (ROS) generation. Antitumor agent-204 induces apoptosis and induces cell cycle arrest at G2/M phase. Antitumor agent-204 shows antitumor activity .
|
-
- HY-150511
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity .
|
-
- HY-146311
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-16 (compound 5g) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-16 shows most potent against cancer cells, with IC50 values of 0.084-0.221 μM. Tubulin polymerization-IN-16 potently disrupts microtubule/tubulin dynamics, induces cell cycle arrest at G2/M phase in SGC-7901 cells .
|
-
- HY-179521
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK1-IN-8 is a CDK1 inhibitor. CDK1-IN-8 inhibits cell migration, induces apoptosis, and arrests the cell cycle at the G2/M phase. CDK1-IN-8 leads to a significant downregulation of CDK1 protein levels in HepG2 cells. CDK1-IN-8 can be used for the study of hepatocellular carcinoma .
|
-
- HY-147949
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
SKLB0565 is a potent tubulin inhibitor. SKLB0565 shows significant anti-proliferative activity against CRC (colorectal carcinoma) cell lines, with IC50 values ranging from 0.012 μM to 0.081 μM. SKLB0565 causes G2/M phase arrest and mitochondria-mediated intrinsic apoptosis. SKLB0565 inhibits cell migration and disrupted the tube formation of HUVECs .
|
-
- HY-178969
-
|
|
FAK
Pyk2
Apoptosis
|
Neurological Disease
Cancer
|
|
GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM) .
|
-
- HY-146006
-
|
|
Microtubule/Tubulin
MMP
|
Cancer
|
|
Tubulin/MMP-IN-1 (compound 15g) is a potent inhibitor of tubulin and MMP. Tubulin/MMP-IN-1 has the potential for the research of cancer diseases. Tubulin/MMP-IN-1 suppresses tubulin polymerization, induces cell cycle arrest at the G2/M phase, leads to reactive oxidative stress (ROS) generation of HepG2 cells, and results in apoptosis by the mitochondrial-dependent apoptotic pathway .
|
-
- HY-157419
-
|
7-(4-Ethylphenyl)-FL118
|
Apoptosis
|
Cancer
|
|
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
|
-
- HY-163707
-
|
|
Apoptosis
|
Cancer
|
|
UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells .
|
-
- HY-115589
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity .
|
-
- HY-169418
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-71 (Compound 4k) is an inhibitor for tubulin polymerization with an IC50 of 3.06 μM. Tubulin polymerization-IN-71 inhibits the proliferation of cancer cell MG-63 and U2OS with IC50 of 0.08-0.14 μM. Tubulin polymerization-IN-71 arrests the cell cycle at G2/M phase, and induces apoptosis in MG-63 .
|
-
- HY-157320
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin/PARP-IN-2 (compound 14) is a dual PARP-Tubulin inhibitor. Tubulin/PARP-IN-2 inhibits PARP1, PARP2, and tubulin activity with IC50 values of 74 nM, 109 nM, and 1.4 µM, respectively. Tubulin/PARP-IN-2 induces apoptosis as well as autophagy. Tubulin/PARP-IN-2 causes cell cycle arrest at the G2/M phase .
|
-
- HY-181664
-
|
|
PARP
Apoptosis
Caspase
|
Cancer
|
|
YCH3971 is a PARP1 inhibitor with a PARP1 IC50 of 7.52 nM and a PARP1 EC50 of 67.75 nM. YCH3971 inhibits the proliferation of BRCA-deficient tumor cells. YCH3971 induces DNA damage, G2/M phase arrest, and caspase-mediated Apoptosis in triple-negative breast cancer cells. YCH3971 can be used for the research of BRCA-deficient tumors .
|
-
- HY-183762
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-68 is a tubulin inhibitor with an IC50 of 19.3 μM. Tubulin-IN-68 exhibits antiproliferative activity against human cancer cells. Tubulin-IN-68 induces G2/M phase cell cycle arrest. Tubulin-IN-68 induces apoptosis. Tubulin-IN-68 can be used in the research of colorectal cancer, hepatocellular carcinoma, breast cancer, and T-cell leukemia .
|
-
- HY-143278
-
|
|
Topoisomerase
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-13 (compound 20) is a potent and effective antileukemic topoisomerase II and FLT3 dual inhibitor with IC50 values of 2.26 μM and 2.26 μM, respectively. FLT3-IN-13 arrests cell cycle at G2/M phase and induce apoptosis. FLT3-IN-13 has anticytotoxic activity, particularly against leukemia .
|
-
- HY-156279
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC6-IN-22 (compound 30) is a inhibitor of HDAC6, with the IC50 of 4.63 nM. HDAC6-IN-22 has antiproliferative effects in vitro and in vivo towards multiple myeloma. HDAC6-IN-22
induces cell cycle arrest in the G2 phase and promotes apoptosis through the mitochondrial pathway .
|
-
- HY-178132
-
|
|
Apoptosis
NF-κB
|
Cancer
|
|
Apoptosis inducer 46 is an apoptosis inducer. Apoptosis inducer 46 exhibits potent and selective growth inhibitory effects on metastatic triple-negative breast cancer (TNBC) cells. Apoptosis inducer 46 induces G2/M phase cell cycle arrest and apoptotic cell death in MDA-MB-231 cells, and blocks NF-κB nuclear translocation. Apoptosis inducer 46 can be used for the study of TNBC .
|
-
- HY-151980
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage .
|
-
- HY-147861
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 11 (compound 3d) is a potent Topoisomerase II inhibitor, with an IC50 of 2.89 μM. Topoisomerase II inhibitor 11 shows 92.46% inhibition on renal cancer cell line A498 with an IC50 of 3.5 μM. Topoisomerase II inhibitor 11 causes cell cycle arrest at the G2/M phase leading to cell proliferation inhibition and pro-apoptotic activity .
|
-
- HY-167237
-
|
|
Apoptosis
Caspase
CDK
PARP
Bcl-2 Family
ERK
|
Cancer
|
|
Calactin is a glycoside that can be isolated from Asclepias curassavica L.. Calactin activates caspase-3, caspase-8, caspase-9, and phosphorylates ERK. Calactin induces DNA damage, apoptosis, PARP cleavage, G2/M phase cell cycle arrest, shifts Bax/Bcl-2 expression, and shows anti-proliferation effects in leukemia cells. Calactin can be used for the research of leukemia .
|
-
- HY-175608
-
|
|
EGFR
Apoptosis
Bcl-2 Family
MDM-2/p53
|
Cancer
|
|
EGFR-IN-171 is an EGFR inhibitor with an IC50 value of 0.19 μM. EGFR-IN-171 also inhibits vascular endothelial growth factor 2 (VEGFR-2) with an IC50 value of 31.65 μM. EGFR-IN-171 can induce apoptosis and G2/M phase cell cycle arrest. EGFR-IN-171 can be used for cancer research, such as liver and breast cancer .
|
-
- HY-183628
-
|
2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine
|
STAT
|
Endocrinology
Cancer
|
|
MEAP (2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine) is a NEDD9-STAT3 modulator. MEAP disrupts NEDD9-STAT3 interaction, driving STAT3 Y705 dephosphorylation. MEAP induces G2/M phase arrest. MEAP can be used for the research of anaplastic thyroid cancer .
|
-
- HY-150582
-
|
|
c-Met/HGFR
c-Kit
FLT3
Apoptosis
|
Cancer
|
|
c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner .
|
-
- HY-B1357R
-
|
|
Reference Standards
Bcl-2 Family
Caspase
Apoptosis
HSV
Na+/K+ ATPase
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
|
-
- HY-149558
-
|
|
Apoptosis
CXCR
|
Cancer
|
|
CXCR4-IN-2 (compound A1) is a bifunctional fluorinated small molecule that is a potent CXCR4 inhibitor with anticancer activity. CXCR4-IN-2 has cytotoxic (IC50: 60 μg/mL; 72 h) and antiproliferative effects on mouse colorectal cancer (CRC) cells. CXCR4-IN-2 induces cell arrest in the G2/M phase and induces apoptosis .
|
-
- HY-N0047R
-
|
|
Reference Standards
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I (Standard) is the analytical standard of Polyphyllin I. This product is intended for research and analytical applications. Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis .
|
-
- HY-146683
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-163371
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR WT/T790M-IN-1 (Compound 16h) is a dual EGFR WT and EGFR T790 inhibitor. EGFR WT/T790M-IN-1 can arrest the cell cycle in G2/M phase and induce apoptosis. EGFR WT/T790M-IN-1 has anti-cancer activity .
|
-
- HY-181717
-
|
|
NF-κB
Apoptosis
Cadherin
Caspase
Bcl-2 Family
|
Neurological Disease
Cancer
|
|
TKL002 is a blood-brain barrier-permeable inhibitor of the CTH/H2S/NF-κB/EMT signaling axis. TKL002 induces G2/M phase cell cycle arrest and apoptosis in glioblastoma cells. TKL002 inhibits the migration and invasion of glioblastoma cells by upregulating E-cadherin and downregulating N-cadherin and vimentin. TKL002 is applicable to relevant research on glioblastoma .
|
-
- HY-181982
-
-
- HY-146682
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-178487
-
|
|
HDAC
DNA/RNA Synthesis
NO Synthase
Apoptosis
|
Cancer
|
|
anti-TNBC agent-12 (Compound 23a) is a multi-target antitumor agent targeting HDAC6 (IC50=30.3 nM), DNA, and inducing nitric oxide (NO) release. anti-TNBC agent-12 induces tumor cell apoptosis and G2/M phase cell cycle arrest. anti-TNBC agent-12 is promising for research of triple-negative breast cancer (TNBC) .
|
-
- HY-157165
-
|
|
Microtubule/Tubulin
PARP
|
Cancer
|
|
Tubulin/PARP-IN-1 (compound 14) is a dual PARP-tubulin inhibitor with activity against endometrial cancer. Tubulin/PARP-IN-1 inhibits PARP and tubulin with IC50s of 74 nM (PARP1), 109 nM (PARP2), and 1.4 μM (Microtubule/Tubulin), respectively. Tubulin/PARP-IN-1 can induce apoptosis and autophagy and cause cell cycle arrest in the G2/M phase .
|
-
- HY-B1295R
-
|
Litarex tetrahydrate (Standard)
|
Apoptosis
Endogenous Metabolite
Bacterial
Reference Standards
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Lithium citrate (tetrahydrate) (Standard) is the analytical standard of Lithium citrate (tetrahydrate). This product is intended for research and analytical applications. Lithium citrate (Litarex) tetrahydrate is a natural preservative and food tartness enhancer. Lithium citrate tetrahydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Lithium citrate tetrahydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Lithium citrate tetrahydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-W009156R
-
|
Potassium citrate monohydrate (Standard)
|
Reference Standards
Apoptosis
Endogenous Metabolite
Bacterial
|
Infection
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid tripotassium hydrate (Standard) (Potassium citrate monohydrate (Standard)) is the analytical standard of Citric acid tripotassium hydrate (HY-W009156). This product is intended for research and analytical applications. Citric acid tripotassium hydrate is a natural preservative and food tartness enhancer. Citric acid tripotassium hydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid tripotassium hydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid tripotassium hydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-117688
-
|
|
HDAC
Topoisomerase
Apoptosis
|
Cancer
|
|
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .
|
-
- HY-W724319
-
|
Sodium citrate-d4; Trisodium citrate anhydrous-d4
|
Isotope-Labeled Compounds
Apoptosis
Bacterial
Endogenous Metabolite
|
Cardiovascular Disease
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Citric acid-d4 trisodium (Sodium citrate-d4) is the deuterium labeled Citric acid trisodium (HY-B2201). Citric acid trisodium (Sodium citrate) is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-174254
-
|
|
Akt
Apoptosis
Caspase
PARP
β-catenin
|
Cancer
|
|
AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells .
|
-
- HY-148595
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1A1-IN-2 (Compound 14) is a competitive inhibitor of CYP1A1 (Ki: 1.4 μM). CYP1A1-IN-2 exhibits potent antimitotic activity and arrests cell in the G2/M phase. CYP1A1-IN-2 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells .
|
-
- HY-150540
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research .
|
-
- HY-178431
-
|
|
mTOR
Apoptosis
Reactive Oxygen Species (ROS)
STING
|
Cancer
|
|
MT-44 is a highly selective and potent mTOR inhibitor with an IC50 of 49.4 nM. MT-44 can inhibit cancer cells proliferation, migration and invasion. MT-44 can induce cells apoptosis and ROS production and cause G2/M phase arrest. MT-44 can activate the cGAS/STING pathway. MT-44 can be used for the research of cancer, such as triple-negative breast cancer .
|
-
- HY-175866
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase-IN-8 is a orally active Aurora kinase inhibitor. Aurora kinase-IN-8 shows IC50 values of 2.8 and 28.1 nM against Aurora A kinase and Aurora B kinase. Aurora kinase-IN-8 can prevent spindle formation, cause G2/M phase arrest, and induce cell apoptosis. Aurora kinase-IN-8 can be used for the research of cancer, such as triple-negative breast cancer .
|
-
- HY-181030
-
|
|
Polo-like Kinase (PLK)
Apoptosis
CDK
Bcl-2 Family
|
Cancer
|
|
BDE30671203 is a highly selective PLK1 inhibitor (IC50 = 2.163 nM). BDE30671203 induces G2/M phase arrest and Apoptosis. BDE30671203 downregulates key cell cycle regulators (CDC20, CDK1) and the anti-apoptotic gene Bcl-2. BDE30671203 exhibits anticancer activity against non-small cell lung cancer, large cell lung cancer, and liver cancer .
|
-
- HY-161501
-
|
|
GLUT
Topoisomerase
Apoptosis
|
Cancer
|
|
3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. 3-Fluoro-evodiamine glucose activates the expression of glucose transporter 1 (GLUT1), and inhibits topoisomerase I/II. 3-Fluoro-evodiamine glucose induces apoptosis and arrests the cell cycle at G2/M phase. 3-Fluoro-evodiamine glucose exhibits antitumor efficacy in vivo and in vitro, without significant toxicity .
|
-
- HY-10180A
-
|
|
Aurora Kinase
|
Cancer
|
|
MLN8054 sodium is an Aurora A inhibitor with radiosensitivity-enhancing activity. MLN8054 sodium can activate the DNA double-strand break reaction of prostate cancer cells in in vitro experiments. The application of MLN8054 sodium is closely related to accumulation in the G2/M phase of the cell cycle and polyploid formation. In vivo experiments show that MLN8054 sodium can significantly delay the growth of prostate cancer tumors and promote tumor cell apoptosis when used in combination with radiotherapy .
|
-
- HY-118529
-
|
|
Phosphatase
|
Cancer
|
|
JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1 .
|
-
- HY-147839
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-175567
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apoptosis inducer 41 is an apoptosis inducer that induces apoptosis through the mitochondrial pathway. Apoptosis inducer 41 exhibits remarkable inhibitory effects against MCF-7 cells (IC50 = 6.2 μM). Apoptosis inducer 41 significantly arrests MCF-7 cells in the G2/M phase, increases ROS accumulation, induces mitochondrial membrane potential depolarization. Apoptosis inducer 41 can used for the study of breast cancer .
|
-
- HY-143660
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
LG308 is a novel synthetic compound with antimicrotubule activity. LG308 induces mitotic phase arrest and inhibits G2/M progression significantly which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. LG308 also induces apoptosis and cell death. LG308 significantly suppresses tumor growth. LG308 with antimitotic activity has the potential for the research of prostate cancer .
|
-
- HY-N12124
-
|
Monascinol
|
Akt
mTOR
AMPK
Androgen Receptor
Apoptosis
Autophagy
|
Cancer
|
|
Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
|
-
- HY-168655
-
|
|
Apoptosis
EGFR
VEGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-146792
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
|
-
- HY-100789R
-
|
|
Apoptosis
Polo-like Kinase (PLK)
Mitosis
Reference Standards
|
Cancer
|
|
ON1231320 (Standard) is the analytical standard of ON1231320 (HY-100789). This product is intended for research and analytical applications. ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 μM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity .
|
-
- HY-175848
-
|
|
c-Met/HGFR
STAT
Apoptosis
Akt
VEGFR
Bcl-2 Family
MDM-2/p53
Caspase
|
Cancer
|
|
NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer .
|
-
- HY-146817
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 μM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
|
-
- HY-12286
-
|
|
Proteasome
Apoptosis
Autophagy
Caspase
Bcl-2 Family
NF-κB
PARP
|
Cancer
|
|
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α .
|
-
- HY-179160
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-61 is a tubulin polymerization inhibitor with an IC50 of ≤7.63 μM. Tubulin-IN-61 induces early apoptosis and triggers significant G2/M phase arrest. Tubulin-IN-61 elevates intracellular ROS levels. Tubulin-IN-61 shows high activity against MCF-7 cells with an IC50 of 5.61 μM. Tubulin-IN-61 can be used for the research of breast cancer .
|
-
- HY-W749442
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
7a-Hydroxyfrullanolide has anticancer properties. 7a-Hydroxyfrullanolide reduces polymerization of α-, β-tubulin. 7a-Hydroxyfrullanolide preferrs to bind to β-tubulin over α-tubulin. 7a-Hydroxyfrullanolide also triggers DNA damage response arrests cells in the G2/M-phase. 7a-Hydroxyfrullanolide is an eudesmanolide sesquiterpene lactone (SL) and can be isolated from the flowering plants of the Asteraceae family .
|
-
- HY-123255
-
|
|
Proteasome
MMP
Apoptosis
Autophagy
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
BSc2118 is a 20S proteasome inhibitor with an IC50 of approximately 50 nM. BSc2118 induces G2/M phase cell cycle arrest and apoptosis in myeloma cells, inhibits cytoprotective autophagy, and suppresses tumor angiogenesis. BSc2118 reduces MMP9 activity, promotes angioneurogenesis, and alleviates recombinant tissue-type plasminogen activator-induced cerebral toxicity. BSc2118 is applicable to studies related to cerebral ischemia and multiple myeloma .
|
-
- HY-169882A
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 49 (Compound 18) hydrobromide is an inhibitor for tubulin polymerization with an IC50 of 48 μM. Tubulin inhibitor 49 hydrobromide disrupts the cell microtubule network, arrests the cell cycle at G2 phase, and exhibits cytotoxicity (IC50=8.8 μM in HeLa cell). Tubulin inhibitor 49 hydrobromide can be used in the research of cervical cancer .
|
-
- HY-149371
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC6-IN-16 (compound 5c) is a histone deacetylase 6 (HDAC6) inhibitor, based on Quinazolin-4(3H)-One. HDAC6-IN-16 exhibits anticancer effect, inhibits colony-forming. And HDAC6-IN-16 arrests cell cycle at G2 phase and induces apoptosis .
|
-
- HY-125677
-
|
|
Caspase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
SHetA2 is a derivative of heteroarotinoid, that exhibits cytotoxicity in cancer cells with IC50 of 0.37–4.6 μM. SHetA2 regulates cancer cells differentiation, induces apoptosis through the intrinsic mitochondrial pathway, and arrest cell cycle at G2 phase. SHetA2 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice. SHetA2 is orally active .
|
-
- HY-118447
-
|
|
CDK
Survivin
|
Cancer
|
|
RO0505124 is a selective CDK4 inhibitor with an IC50 of 20 nM. RO0505124 reversibly binds the ATP pocket of the kinase. RO0505124 induces G1 phase arrest in cancer cells via reduced retinoblastoma protein (Rb) phosphorylation, blocking S phase progression. RO0505124 exhibits anti-proliferative activity against various cancer cells. RO0505124 delays mitotic entry, induces aberrant mitosis with lagging chromosomes, driving mitotic slippage and formation of multinucleated or micronucleated cells. RO0505124 inhibits G2/M phase accumulation of survivin and borealin. RO0505124 can be used for the research of cancer .
|
-
- HY-180838
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
WW-104 is a selective USP10 inhibitor with an IC50 of 16.75 μM, a Kd of 237 nM. WW-104 induces the G2 phase arrest and cell Apoptosis. WW-104 exhibits significant anti-proliferative effects across USP10-overexpressing cell lines. WW-104 has anti-cancer effects against hepatocellular carcinoma .
|
-
- HY-151436
-
|
|
CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
|
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
|
-
- HY-180147
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Microtubule-IN-14 (Compound 10u) is a microtubule inhibitor. Microtubule-IN-14 inhibits the polymerization of tubulin, thereby preventing the formation of the spindle apparatus in cell mitosis and blocking the cell cycle at the G2/M phase. Microtubule-IN-14 induces a decrease in mitochondrial membrane potential and a burst of reactive oxygen species (ROS), promoting tumor cell apoptosis. Microtubule-IN-14 can be used for the study of non-small cell lung cancer and liver cancer .
|
-
- HY-149029
-
|
|
HDAC
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
TH-6 is a potent HDAC inhibitor with IC50s of 0.115, 0.135, 0.242, 0.138, 2.120 µM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively. TH-6 inhibits cell migration and invasion. TH-6 induces apoptosis and cell cycle arrest at G2/M phase. TH-6 shows anti-tumor activity .
|
-
- HY-172880
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK1-IN-15 (Compound 7n) is a PLK1 inhibitor (IC50: 38.5 nM). PLK1-IN-15 exhibits antiproliferative activity against HepG2, Huh7, H1299 and A549 cells (IC50: 2.03, 2.08, 4.79 and 17.11 μM, respectively). PLK1-IN-15 induces cell cycle arrest at the G2/M phase and apoptosis, and has anticancer activity .
|
-
- HY-146392
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
HDAC-IN-39 (compound 16c) is a potent HDAC inhibitor, with IC50 values of 1.07 μM (HDAC1), 1.47 μM (HDAC2), and 2.27 μM (HDAC3), respectively. HDAC-IN-39 also significantly inhibits microtubule polymerization. HDAC-IN-39 induces cell cycle arrest at the G2/M phase. HDAC-IN-39 displays promising anticancer activity against resistant cancer cells .
|
-
- HY-177268
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
PARP
Caspase
Akt
|
Cancer
|
|
CHNQD-01426 (Compound 4a) is an anticancer agent. CHNQD-01426 has cytotoxic activities against cancer cells. CHNQD-01426 significantly inhibits hepatocellular carcinoma cells proliferation via arresting S and G2/M phase cell cycle and induces apoptosis by inducing ROS production and elevating apoptosis-related proteins expression. CHNQD-01426 potently inhibits tumor growth in HepG2 xenograft mice model .
|
-
- HY-178005
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-151984
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity .
|
-
- HY-N2983
-
|
|
Tyrosinase
|
Others
|
|
Cajanin is a potent and orally active anti-melanogenic agent. Cajanin shows antiproliferative activity in MNT1 Cells. Cajanin efficiently decreases the melanin content. Cajanin down-regulates the mRNA and protein expression levels of MITF, tyrosinase, TRP-1 and Dct (TRP-2). Cajanin induces cell cycle arrest at G2/M and S phase. Cajanin stimulates osteoblast proliferation. Cajanin has the potential for the research of human hyperpigmented disorders and menopausal osteoporosis .
|
-
- HY-124122
-
|
|
VEGFR
Checkpoint Kinase (Chk)
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases .
|
-
- HY-179516
-
|
|
Akt
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
AKT1-IN-11, a Podophyllotoxin (HY-15552) derivative, is a AKT1/tubulin dual inhibitor. AKT1-IN-11 down-regulates the phosphorylation level of AKT kinase in tumor cells, disrupting cell proliferation, causeing G2/M phase arrest and inducing apoptosis. AKT1-IN-11 also promotes tubulin depolymerization. AKT1-IN-11 can be used for the research of colorectal cancer .
|
-
- HY-146444
-
|
|
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9 .
|
-
- HY-146261
-
|
|
Microtubule/Tubulin
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
|
Cancer
|
|
HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer .
|
-
- HY-146228
-
|
|
HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
|
Cancer
|
|
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
|
-
- HY-173074
-
|
|
Microtubule/Tubulin
MDM-2/p53
Apoptosis
|
Cancer
|
|
Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460 .
|
-
- HY-15149S2
-
|
FK 228-d7; FR 901228-d7; NSC 630176-d7
|
Isotope-Labeled Compounds
HDAC
Apoptosis
|
Cancer
|
|
Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
|
-
- HY-161372
-
|
|
PARP
c-Met/HGFR
Apoptosis
|
Cancer
|
|
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
|
-
- HY-400684
-
|
|
Bacterial
|
Cancer
|
|
Tubulysin A intermediate-1 is an intermediate in the synthesis of the cytotoxic peptide Tubulysin A (HY-15995). Tubulysin A (TubA) is an antibiotic, anti-microtubule toxins, and apoptosis inducer isolated from myxobacteria. Tubulysin A has anti-angiogenic, anti-microtubule, anti-mitotic, and anti-proliferative activities. Tubulysin A arrests cells in the G2/M phase, effectively inhibits tubulin polymerization, and induces depolymerization of detached microtubules. Tubulysin A acts as an ADC cytotoxin (ADC Cytotoxin) to synthesize ADC .
|
-
- HY-W011762
-
|
|
Apoptosis
|
Cancer
|
|
VK3-OCH3 is a potent antitumor agent. VK3-OCH3 shows cytotoxicity for neuroblastoma cell lines and low cytotoxicity for normal cell lines. VK3-OCH3 induces apoptosis and cell cycle arrest at G2/M phase in IMR-32 cells. VK3-OCH3 shows antitumor activity .
|
-
- HY-162000
-
|
|
Apoptosis
|
Cancer
|
hCAIX/XII-IN-13 is an inhibitor of human carbonic anhydrases (hCA). hCAIX/XII-IN-13 shows good inhibitory activity against the tumor-related CA subtypes IX and XII, with Ki values of 0.08 µM and 0.06 µM, respectively. Under hypoxic conditions, hCAIX/XII-IN-13 can restore the cytotoxicity of Doxorubicin (HY-15142A) on MCF-7 cells, increasing G2/M phase cell cycle arrest and apoptosis .
|
-
- HY-144293
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma .
|
-
- HY-N13063
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
PI3K
Akt
|
Cancer
|
|
Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 .
|
-
- HY-179054
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
|
|
Apoptosis inducer 51 (Compound 5d) is an apoptosis inducer. Apoptosis inducer 51 exhibits strong inhibitory activity against MDA-MB-231 cells. Apoptosis inducer 51 inhibits cell invasion and migration, induces G2/M phase cell cycle arrest and cell apoptosis. Apoptosis inducer 51 causes DNA damage, ROS burst and mitochondrial membrane potential (MMP) collapse. Apoptosis inducer 51 can be used for the study of triple-negative breast cancer.
|
-
- HY-156182
-
|
|
JNK
Cytochrome P450
|
Cancer
|
|
JNK-IN-14 is a potent JNK inhibitor with IC50 values of 1.81, 12.7 and 10.5 nM for JNK1, JNK2 and JNK3, respectively. JNK-IN-14 induces early-stage apoptosis. JNK-IN-14 shows cell population arrest at the G2/M phase and slightly inhibits beclin-1 production at K562 leukemia cells relative to SP600125 (HY-12041), showing higher inhibitory ability.
|
-
- HY-159938
-
|
|
p38 MAPK
Apoptosis
Bcl-2 Family
MDM-2/p53
Caspase
|
Cancer
|
|
p38α inhibitor 6 (compound 19) is a p38α inhibitor with the IC50 of 0.68 μM. p38α inhibitor 6 induces cell apoptosis and arrests cell cycle at G0 and G2/M phase. p38α inhibitor 6 decreases the TNF-α concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7 .
|
-
- HY-N9778
-
|
|
Apoptosis
Bcl-2 Family
Caspase
Drug Derivative
|
Cancer
|
|
Phoyunbene B is a similar substance to Resveratrol (HY-16561). Phoyunbene B exhibits stronger growth inhibitory activity against human liver cancer cells HepG2 compared to Resveratrol. Phoyunbene B induces G2/M phase cell cycle arrest and apoptosis. Phoyunbene B increases Bax/Bcl-2 and activates Caspase-3. Phoyunbene B inhibits the invasion and migration of cancer cells. Phoyunbene B can be used for research on liver cancer .
|
-
- HY-180148
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Microtubule-IN-15 (Compound 10v) is a microtubule inhibitor. Microtubule-IN-15 inhibits the polymerization of tubulin, thereby preventing the formation of the spindle apparatus in cell mitosis and blocking the cell cycle at the G2/M phase. Microtubule-IN-15 induces a decrease in mitochondrial membrane potential and a burst of reactive oxygen species (ROS), promoting tumor cell apoptosis. Microtubule-IN-15 can be used for the study of non-small cell lung cancer and liver cancer .
|
-
- HY-170568
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
|
-
- HY-156088
-
|
|
Apoptosis
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
SSE1806 is a derivative of podophyllotoxin (a natural antimitotic agent) and a microtubule/tubulin inhibitor with significant anticancer and antiproliferative activities. The GI50 of SSE1806 on cancer cell growth ranges from 1.29-21.15 μM. SSE1806 causes mitotic abnormalities and G2/M phase arrest, increases p53 expression, and inhibits colon cancer organoid growth. SSE1806 is able to overcome multidrug resistance in cell lines overexpressing MDR-1 .
|
-
- HY-155780
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-173166
-
|
|
PPAR
|
Cancer
|
|
PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier .
|
-
- HY-175811
-
|
|
Ferroptosis
Glutathione Peroxidase
|
Cancer
|
|
Ferroptosis inducer-10 is a ferroptosis inducer. Ferroptosis inducer-10 can inhibit A549 cells growth with an IC50 of 0.76 μM. Ferroptosis inducer-10 can deplete GSH, elevate ROS and MDA, and downregulate GPX4 expression. Ferroptosis inducer-10 can induce cell G2/M phase and inhibit migration. Ferroptosis inducer-10 can be used for the research of cancer, such as non-small lung cancer .
|
-
- HY-179695
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
|
Cancer
|
|
Microtubule destabilizing agent-3, a B32B3 (HY-12240) analog, is a microtubule destabilizing agent. Microtubule destabilizing agent-3 exerts its antimyeloma phenotypes by destabilizing microtubules and promoting mitotic arrest, leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis. Microtubule destabilizing agent-3 can be used for the research of multiple myeloma .
|
-
- HY-118385
-
|
|
Microtubule/Tubulin
|
Cancer
|
ER-67880 is a potent microtubule inhibitor with an IC50 of 9.5 μM. ER-67880 exhibits anti-proliferative activity against KB, Colon 38 and P338 cells with IC50s of 0.55, 0.2 and 0.76 μg/mL. ER-67880 causes G2/M phase arrest and is accompanied by abnormal DNA replication. ER-67880 exhibits a down-regulation pattern of G1 phase-related genes. ER-67880 can be used in various cancer studies, including those of nasopharyngeal carcinoma and murine adenocarcinoma .
|
-
- HY-N4327
-
|
|
NF-κB
Apoptosis
Akt
Bcl-2 Family
|
Infection
Inflammation/Immunology
|
|
Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394) .
|
-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
|
-
- HY-N15306
-
|
|
Apoptosis
|
Cancer
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-130559
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
SL-3-19 is a tubulin ligand. SL-3-19 exhibits antitumor activity against esophageal squamous cell carcinoma (ESCC) both in vitro and in vivo by inhibiting microtubule assembly, inducing G2/M phase cell cycle arrest and apoptosis, and disrupting tumor blood vessels. SL-3-19 has a higher activity than SL-1-73 (HY-130558). SL-3-19 can be used for the research of ESCC and other tumors .
|
-
- HY-N0168
-
|
|
p38 MAPK
Autophagy
Apoptosis
Reactive Oxygen Species (ROS)
NF-κB
Bcl-2 Family
|
Neurological Disease
Cancer
|
|
Hesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor .
|
-
- HY-183581
-
|
|
Deubiquitinase
DNA/RNA Synthesis
|
Cancer
|
|
USP1-IN-18 is an orally active USP1 inhibitor with a human IC50 of 17.0 nM. USP1-IN-18 inhibits USP1-UAF1 deubiquitinase activity and drives ubiquitinated PCNA accumulation. USP1-IN-18 induces DNA damage, replication stress, and G2-M phase cell cycle arrest. USP1-IN-18 can be used for the research of triple-negative breast cancer .
|
-
- HY-183334
-
|
|
Phosphodiesterase (PDE)
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
TDP1-IN-5 is a tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 2.2 μM. By targeting TDP1 both intracellularly and extracellularly, TDP1-IN-5 inhibits the NHEJ repair pathway, arrests the cell cycle at the G2/M phase, upregulates PIG3 to enhance ROS, and ultimately significantly potentiates ionizing radiation (IR)-induced DNA damage and apoptosis. TDP1-IN-5 can be used in the research of colorectal cancer .
|
-
- HY-161302
-
|
|
Apoptosis
DNA/RNA Synthesis
PARP
|
Cancer
|
|
Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity .
|
-
- HY-180196
-
|
|
EGFR
Bcl-2 Family
CDK
Atg8/LC3
Apoptosis
Autophagy
|
Cancer
|
|
EGFR-IN-187 (Compound 4d) is a selective EGFR inhibitor with an IC50 of 25.41 μM. EGFR-IN-187 can cause cancer cells S amd G2/M phase arrest and induce apoptosis and autophagy. EGFR-IN-187 upregulates CCNE1, Bax, LC3B-II and P27 expression and downregulates CCNA1 and Bcl-2 levels. EGFR-IN-187 can be used for the research of cancer, such as lung cancer .
|
-
- HY-150795
-
|
|
TGF-beta/Smad
PI3K
Akt
ERK
JNK
|
Others
|
|
SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. SY-LB-35 can stimulate significant increases in cell number and cell viability in the C2C12 myoblast cell line, and causes shifts towards the S and G2/M phases of the cell cycle. SY-LB-35 stimulates canonical Smad and non-canonical PI3K/Akt, ERK, p38 and JNK intracellular signaling pathways .
|
-
- HY-181019
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
|
Neurological Disease
Cancer
|
|
iMPZ-8 is a β-tubulin polymerization inhibitor that inhibits β-tubulin protein expression, disrupts microtubule structure, impairs microtubule organization. iMPZ-8 inhibits proliferation and reduces cellular migration and colonization in cancer cells. iMPZ-8 induces G2/M phase arrestand induces apoptosis via the BAX-Caspase-3 intrinsic apoptotic signaling pathway. iMPZ-8 can be used for the research of cancer, suah as breast cancer, neuroblastoma and colon cancer .
|
-
- HY-N13294
-
|
TMJ-105
|
Apoptosis
JAK
STAT
p38 MAPK
JNK
ERK
|
Cancer
|
|
Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC50 value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy .
|
-
- HY-13442C
-
|
B1939 mesylate (purity>99%, single impurity ≤ 0.15%); E7389 mesylate (purity>99%, single impurity ≤ 0.15%); ER-086526 mesylate (purity>99%, single impurity ≤ 0.15%)
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Eribulin (B1939; E7389; ER-086526) mesylate (purity>99%, single impurity ≤ 0.15%) is an inhibitor for microtubule. Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate (purity>99%, single impurity ≤ 0.15%) exhibits antitumor efficacy in mouse model .
|
-
- HY-179016
-
|
|
Ferroptosis
Apoptosis
Mitochondrial Metabolism
Calcium Channel
|
Cancer
|
|
Ferroptosis/apoptosis inducer-3 (Compound 34) is a Ferroptosis and Apoptosis inducer. Ferroptosis/apoptosis inducer-3 induces both Ferroptosis and Apoptosis by causing G2/M phase cell cycle arrest, disrupting mitochondrial membrane potentials, promoting lipid peroxidation, and increasing the levels of Ca 2+ and Fe 2+ through the activation of calcium/calmodulin signaling. Ferraplasm/apoptosis inducer-3 shows anticancer effects against cervical cancer, adenocarcinoma, breast cancer, colon cancer, and colorectal carcinoma .
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-
- HY-147947
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
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-
- HY-175175
-
|
|
p38 MAPK
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
PARP
Apoptosis
|
Cancer
|
|
MAPK-IN-5 is a potent MAPK inhibitor with an IC50 of 1.35 μM against HeLa cells. MAPK-IN-5 inhibits HeLa cell proliferation by inducing ROS-mediated DNA damage and mitochondrial apoptosis via the MAPK pathway. MAPK-IN-5 significantly inhibits colony formation, reduces the number of live cells, suppresses cell migration, and causes cell cycle arrest in the G2/M phase in HeLa cells. MAPK-IN-5 can be used for the study of cervical cancer .
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-
- HY-180449
-
|
|
Microtubule/Tubulin
Wnt
|
Cancer
|
|
Anticancer agent 291 (Compound 2406) is an anti-cancer agent. Anticancer agent 291 interferes with the integrity of the β-tubulin cytoskeleton and inhibits the Wnt/β-catenin signal transduction. Anticancer agent 291 significantly inhibits the invasion, migration and colony formation of tumor cells. Anticancer agent 291 induces the cell cycle of EC-9706 and HT-29 cells to arrest at the G2/M phase and inhibits cell proliferation. Anticancer agent 291 can be used for the study of gastrointestinal cancer .
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-
- HY-N14734
-
|
|
Apoptosis
Fungal
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
Disorazol A1 is an tubulin inhibitor with antifungal activity. Disorazol A1 functions by inhibiting tubulin polymerization, interfering with microtubule formation, blocking mitosis, thus arresting the cell cycle at the G2/M phase and inducing apoptosis. Disorazol A1 also exhibits an inhibitory effect against L929 mouse fibroblasts with an IC50 value of 3 pM. Disorazol A1 causes the accumulation of p53 protein in the cell nucleus. Disorazol A1 is promising for research of cancers .
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-
- HY-103257R
-
|
NSC656158 (Standard)
|
Reference Standards
Microtubule/Tubulin
|
Cancer
|
|
CHM-1 (Standard) is the analytical standard of CHM-1 (HY-103257). This product is intended for research and analytical applications. CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity .
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-
- HY-170402
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
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-
- HY-182986
-
|
|
CDK
Apoptosis
DNA/RNA Synthesis
Aurora Kinase
|
Cancer
|
|
LS-Q2 is a highly selective CDK4/9 inhibitor with IC50 values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors .
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-
- HY-163692
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549 .
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-
- HY-151443
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-180893
-
|
|
Wee1
Apoptosis
|
Cancer
|
|
XH-30 is a potent, selective, and orally active PKMYT1 inhibitor, with an IC50 of 4.1 nM. XH-30 suppresses the proliferation of P53-mutated triple-negative breast cancer (TNBC) cells by inducing G2/M phase release, DNA damage, and apoptosis. XH-30 demonstrates antitumor effects in an MDA-MB-231 mouse model. XH-30 can be used for P53-mutated TNBC research .
|
-
- HY-124211
-
|
|
Environmental Pollutants
MDM-2/p53
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Dibenzo (a,i) pyrene is a polycyclic aromatic hydrocarbon and also a carcinogenic ligand of the TCDD (Ah) receptor. Dibenzo (a,i) pyrene binds to the TCDD (Ah) receptor in rat liver. Dibenzo (a,i) pyrene induces DNA adduct formation and upregulates the protein levels of p53 and p21 WAF1 in diploid lung fibroblasts. Dibenzo (a,i) pyrene alters the cell cycle distribution of diploid lung fibroblasts, increasing the proportion of cells in the S phase, decreasing the proportions of cells in the G0/G1 and G2/M phases, and causing S phase delay/arrest. Dibenzo (a,i) pyrene is applicable for cancer research .
|
-
- HY-105409
-
|
NVP-XAA-296; XAA 296
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Discodermolide (NVP-XAA-296) is a potent microtubule-stabilizing agent with a Ki of 0.4 μM. Discodermolide stabilizes microtubules, induces G2 or M phase cell cycle arrest and apoptosis, leading to inhibition of cancer cell proliferation. Discodermolide competitively inhibits the binding of Paclitaxel (HY-B0015) to tubulin polymers, and inhibits the growth of Paclitaxel-resistant cells. Discodermolide can be used for breast and colon cancer research .
|
-
- HY-175265
-
|
|
c-Myc
Ras
Apoptosis
|
Cancer
|
|
PQ32 is an antitumor agent that targets c-MYC Pu27 and KRAS G-quadruplexes. PQ32 inhibits tumor cell proliferation, arrests the cell cycle at the G2 phase, and induces apoptosis. PQ32 inhibits the expression of c-MYC and KRAS genes. PQ32 can inhibit tumor growth in mice and is used in the study of lymphoma, breast cancer, lung cancer, hepatocellular carcinoma, colorectal cancer, and other cancers .
|
-
- HY-161868
-
|
|
PARP
HDAC
Apoptosis
|
Cancer
|
|
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
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-
- HY-149912
-
|
|
Polo-like Kinase (PLK)
Trk Receptor
Apoptosis
|
Cancer
|
|
CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC50=2.6 nM). CZS-241 inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
|
-
- HY-168565
-
|
|
Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
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-
- HY-146432
-
|
|
Apoptosis
Raf
Ras
ROS Kinase
MDM-2/p53
|
Cancer
|
|
Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model .
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-
- HY-176217
-
|
|
Biochemical Assay Reagents
DNA/RNA Synthesis
|
Cancer
|
|
dA-NHbenzylOCF3 is a DNA-targeted radiosensitizer that enhances the sensitivity of tumor cells to X-rays through the dissociative electron attachment (DEA) mechanism. dA-NHbenzylOCF3 has low toxicity to normal cells and is mainly localized in the cytoplasm and nucleus after entering the cell. dA-NHbenzylOCF3 exerts radiosensitization effects by inducing cell cycle arrest in the radiosensitive G2/M phase. dA-NHbenzylOCF3 can be used for radiosensitization studies of malignant tumors such as prostate cancer and breast cancer .
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-
- 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-163661
-
|
|
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity .
|
-
- HY-172617
-
|
|
BMI1
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
APD-94 is a dual inhibitor targeting tubulin and Bmi-1. APD-94 interfers tubulin normal polymerization. APD-94 suppresses the expression of Bmi-1. APD-94 causes cell cycle arrest at the G2/M phase in cancer cells and induces apoptosis, thus inhibiting cancer cell proliferation. APD-94 represses the growth of HT29 cell xenografts in NOD/SCID mice. APD-94 can be used for colorectal cancer study .
|
-
- HY-157543
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-59 is a tubulin polymerization inhibitor and colchicine binding site inhibitor (CBSI) (IC50 = 6.1 μM). Tubulin polymerization-IN-59 exerts potent antiproliferative activity against cancer cells, while showing lower cytotoxicity to normal cells. Tubulin polymerization-IN-59 arrests colorectal cancer HCT 116 cells in G2/M phase, induces cell apoptosis, and suppresses tumor cell colony formation and migration. Tubulin polymerization-IN-59 can be used for the study of colorectal cancer (CRC) .
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-
- HY-161644
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-27 (Compound 41) is an orally active inhibitor for phosphorylation of STAT3 (KD is 4.4 μM) and STAT3 transcription (IC50 is 22.57 nM). STAT3-IN-27 inhibits proliferation of various cancer cells with IC50 of 10-500 nM. STAT3-IN-27 arrests the cell cycle at G2/M phase, induces mitochondrial dysfunction and apoptosis in HCT116, inhibits cell migration of HCT116. STAT3-IN-27 exhibits antitumor efficacy in mouse model .
|
-
- HY-172088
-
|
|
Microtubule/Tubulin
MMP
NF-κB
Apoptosis
|
Cancer
|
|
Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC50 of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models .
|
-
- HY-P991501
-
|
HcHAb18
|
ADC Antibody
Transmembrane Glycoprotein
SARS-CoV
|
Infection
Cancer
|
|
Meplazumab (HcHAb18) is a humanized anti-CD147 IgG1 antibody a Kd of 0.47 nM. Meplazumab shows anti-SARS-CoV-2 and antitumor activity. Meplazumab conjugated with DM1 can form an antibody-conjugated drug ( HcHAb18-DM1), which induces G2/M phase cell cycle arrest and exerts antiproliferative activity in cancer cells. Meplazumab can be used for the researches of COVID-19 pneumonia and non-small cell lung cancer .
|
-
- HY-144637
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
- HY-N12461
-
|
|
Bacterial
Caspase
Apoptosis
|
Infection
|
|
Cucurbitacin F is a tetracyclic protostane-type triterpenoid with low toxicity, antibacterial and anti-inflammatory activities, and is also a related compound of Cucurbitacin B (HY-N0416). Cucurbitacin F widely exists in plants such as Cucurbitaceae plants, Quisqualis indica and Sorbaria sorbifolia. Cucurbitacin F acts as an actin aggregator and reduces cell viability in a dose-dependent manner. Cucurbitacin F induces apoptosis by triggering G2/M phase cell cycle arrest and activating the caspase-3-dependent apoptosis .
|
-
- HY-178350
-
|
|
CDK
HDAC
Apoptosis
Histamine Receptor
|
Cancer
|
|
MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer .
|
-
- HY-126876
-
GL-V9
1 Publications Verification
|
Apoptosis
AMPK
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model .
|
-
- HY-146138
-
|
|
EGFR
VEGFR
Casein Kinase
Topoisomerase
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
EGFR-IN-57 (Compound 25a) is a potent, orally active EGFR-TK inhibitor with an IC50 of 0.054 µM. EGFR-IN-57 also inhibits VEGFR-2, CK2α, topoisomerase IIβ and tubulin polymerization with IC50 values of 0.087, 0.171, 0.13 and 3.61 µM, respectively. EGFR-IN-57 induces cell cycle arrest at G2/M and pre-G1 phases. EGFR-IN-57 induces cancer cell apoptosis .
|
-
- HY-155852
-
|
|
Ferroptosis
Apoptosis
ACSL Family
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
Lepadin H is a ferroptosis inducer and apoptosis inducer with in vitro cytotoxicity and in vivo antitumor efficacy against cancer cells. Lepadin H reduces GPX4 and SLC7A11 levels, increases p53 and ACSL4 expression, drives lipid hydroperoxide production, elevates reactive oxygen species (ROS) levels, reduces cellular glutathione (GSH) levels, induces lipid peroxidation and G2/M phase cell cycle arrest, and suppresses clonogenic growth and migration of cancer cells.Lepadin H can be used for the research of melanoma .
|
-
- HY-168623
-
|
|
EGFR
Apoptosis
Necroptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
|
|
EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity .
|
-
- HY-173500
-
|
|
MMP
Apoptosis
EGFR
STAT
|
Cancer
|
|
MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer .
|
-
- HY-143462
-
|
|
HDAC
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
|
-
- HY-150772
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
|
-
- HY-179078
-
|
|
OLIG2
Apoptosis
Caspase
PARP
|
Neurological Disease
Cancer
|
|
CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC50 of 1250 nM. CT-179 disrupts OLIG2 dimerization, phosphorylation, and DNA binding, blocking OLIG2-driven transcription. CT-179 induces G2/M phase arrest and increases G0 population. CT-179 induces apoptosis by reducing anti-apoptotic proteins and increasing cleaved caspase-3 and cleaved PARP. CT-179 can be used for the research of subgroup medulloblastoma .
|
-
- HY-179520
-
|
|
Topoisomerase
DNA/RNA Synthesis
MDM-2/p53
Bcl-2 Family
|
Cancer
|
|
XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer .
|
-
- HY-120561
-
|
|
Trk Receptor
IRAK
Pim
Apoptosis
|
Cancer
|
|
PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC50 of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC50 of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-181723
-
|
|
PARP
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Anticancer agent 304 is an anticancer agent. Anticancer agent 304 binds to CDC45 with a Kd value of 83.0 μM. Anticancer agent 304 arrests the cell cycle of liver cancer cells at the G2/M phase, induces Apoptosis by upregulating C-PARP-1 and downregulating PARP-1 and BCL-2, and inhibits the migration, invasion and proliferation of liver cancer cells. Anticancer agent 304 suppresses tumor growth in animal models of hepatocellular carcinoma. Anticancer agent 304 is applicable to research related to liver cancer .
|
-
- HY-170366
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with an IC50 of 42.5 nM. VEGFR-2-IN-58 displays selective cytotoxicity against cancer cells. VEGFR-2-IN-58 shows cellular growth arrest at the G2/M phase in cancer cells. VEGFR-2-IN-58 induces cancer cells Apoptosis, increasing BAX expression and reducing Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells .
|
-
- HY-179385
-
|
|
Microtubule/Tubulin
Phosphatase
Apoptosis
|
Cancer
|
|
Tubulin-IN-62 is a tubulin inhibitor targeting the colchicine-binding site. Tubulin-IN-62 exhibits IC50 values of 17.2 nM and 19.3 nM against SKOV3 and HCC827 cells, respectively. Tubulin-IN-62 inhibits microtubule polymerization, arrests the cell cycle at the G2/M phase, and induces apoptosis. Tubulin-IN-62 demonstrates significant antitumor efficacy in vivo with good tolerability. Tubulin-IN-62 can be used in ovarian cancer and non-small cell lung cancer (NSCLC) research .
|
-
- HY-125542
-
|
|
Apoptosis
JAK
STAT
ERK
PI3K
Akt
|
Cancer
|
|
DCZ3301 is an apoptosis inducer. DCZ3301 modulates JAK2/STAT3, ERK1/2, and PI3K/AKT pathways. DCZ3301 induces G2/M and M phase cell cycle arrest and inhibits cell proliferation and viability. DCZ3301 enhances DNA damage, inhibits DNA repair, and suppresses angiogenesis. DCZ3301 can be used for the research of diffuse large B-cell lymphoma, multiple myeloma and leukemia/lymphoma .
|
-
- HY-175512
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer .
|
-
- HY-182009
-
|
|
DNA Methyltransferase
Apoptosis
Caspase
Mitochondrial Metabolism
|
Cancer
|
|
DNMT-IN-6 is a DNA methyltransferase inhibitor with activity against DNMT1, DNMT3A, and DNMT3B. DNMT-IN-6 drives demethylation, and restores TMS1 tumor suppressor gene expression. DNMT-IN-6 induces apoptosis, causes G2/M phase arrest, disrupts mitochondrial integrity, and activates the intrinsic caspase cascade (3/7/9). DNMT-IN-6 inhibits tumor growth, and improves survival in xenograft models. DNMT-IN-6 can be used for the research of cancer, such as diffuse large B-cell lymphoma .
|
-
- HY-175846
-
|
|
Drug Derivative
Apoptosis
|
Cancer
|
|
TQFL13 is derivative of Thymoquinone (TQ) (HY-D0803) with potent anti-breast cancer activity. TQFL13 exhibits higher cytotoxicity against breast cancer cells (BT549, MDA-MB-231, 4T1). TQFL13 increases apoptosis and blocks the cell cycle at S and G2/G1 phases in breast cancer cells. TQFL13 shows dose-dependent anti-tumor efficacy in mouse breast cancer allograft model. TQFL13 can be used for the study of breast cancer .
|
-
- HY-168718
-
|
|
FAK
JAK
Aurora Kinase
PI3K
Akt
Apoptosis
|
Cancer
|
|
FAK-IN-22 (Compound 26) is an inhibitor of FAK, JAK3, and Aurora B, with IC50 values of 50.94 nM, 9.99 nM, and 0.49 nM, respectively, effectively inhibiting tumor occurrence and metastasis in pancreatic ductal adenocarcinoma (PDAC). FAK-IN-22 effectively inhibits the proliferation of PANC-1 cells, with an IC50 value of 0.15 μM. FAK-IN-22 induces apoptosis and G2/M phase arrest in PANC-1 cells by inhibiting the FAK/PI3K/Akt signaling pathway .
|
-
- HY-153996
-
|
|
Deubiquitinase
Apoptosis
Bcr-Abl
STAT
c-Myc
|
Cancer
|
|
CT1113 is a selective, orally active USP25/USP28 inhibitor. CT1113 inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. CT1113 reduces the levels of total BCR-ABL1, phosphorylated BCR-ABL1, total STAT5, and phosphorylated STAT5, but does not alter the mRNA level of BCR-ABL1. CT1113 is applicable to research related to pancreatic cancer, colon cancer, and acute leukemia .
|
-
- HY-13270
-
|
E7010
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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- HY-183316
-
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Akt
PI3K
PERK
p38 MAPK
ERK
Apoptosis
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Cancer
|
|
Anticancer agent 319 is an anticancer agent. Anticancer agent 319 inhibits the proliferation of liver cancer cells. Anticancer agent 319 inhibits AKT phosphorylation and blocks the PI3K/AKT signaling axis; meanwhile, it inhibits ERK1/2 phosphorylation and blocks the MAPK/ERK signaling axis. Anticancer agent 319 induces G2/M phase cell cycle arrest, triggers apoptosis, and reduces mitochondrial membrane potential in liver cancer cells. Anticancer agent 319 can be used for the research of hepatocellular carcinoma .
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- HY-146276
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HDAC
CDK
Apoptosis
|
Cancer
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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 .
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- HY-N4189
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PI3K
Akt
p38 MAPK
STAT
Apoptosis
|
Cancer
|
Isocucurbitacin B is a natural terpenoid compound found in Pedicellus Melo. Isocucurbitacin B can inhibit the PI3K/AKT, MAPK, and STAT3 signaling pathways and downregulate CAV1 expression. Isocucurbitacin B can inhbit cancer cell proliferation, migration and invision. Isocucurbitacin B can induce apoptosis and cause G2/M phase arrest. Isocucurbitacin B can decrease intracellular cholesterol and PH levels and increase intracellular calcium levels. Isocucurbitacin B can be used for the research of cancer, such as glioma [1][2].
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- HY-170574
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Molecular Glues
Apoptosis
RIO Kinase
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Cancer
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CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .
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- HY-161858
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PI3K
Akt
Apoptosis
|
Cancer
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EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction .
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- HY-130709
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PROTACs
CDK
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Cancer
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PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand .
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- HY-15149G
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FK 228; FR 901228; NSC 630176
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HDAC
Apoptosis
|
Cancer
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|
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
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- HY-N1988
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Hemslecin A
|
Survivin
Apoptosis
EGFR
Caspase
p38 MAPK
Autophagy
MEK
Raf
ERK
STAT
CaMK
|
Inflammation/Immunology
Cancer
|
|
Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC50 of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer .
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-
- HY-155965
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VEGFR
PARP
Apoptosis
|
Cancer
|
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
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-
- HY-179614
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PARP
DNA/RNA Synthesis
Apoptosis
CDK
Bcl-2 Family
|
Cancer
|
|
PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer .
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-
- HY-175522
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|
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P-glycoprotein
Apoptosis
|
Cancer
|
|
P-gp-IN-31 is a P-glycoprotein (P-gp) inhibitor with IC50 values of 0.42 μM for KB cells and 0.43 μM for MDR KBvin cells. P-gp-IN-31 can pass P-gp-mediated drug efflux mechanisms and shows collateral sensitivity via P-gp downregulation. P-gp-IN-31 inhibits cell proliferation, induces apoptosis and arrests the cell cycle at G2/M phase. P-gp-IN-31 can be used for the research of cancer, such as multidrug-resistant (MDR) malignancies .
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-
- HY-168102
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
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-
- HY-178496
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|
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Hsp-targeting Chimeras
PARP
HSP
|
Cancer
|
|
DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC50 = 187 nM). DDO3602 can be used for research on cancer such as breast cancer. (Pink: PARP1 Ligand (HY-75706); Blue: HSP90 Ligand (HY-179203); Black: Linker (HY-W015300))
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-
- HY-150597
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|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
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-
- HY-159936
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|
|
HDAC
PPAR
Apoptosis
|
Cancer
|
|
CS4 is a selective HDAC inhibitor with the IC50 values of 38 nM, 12 nM, 5.8 μM, 19 μM and 61 μM against of HDAC1, HDAC6, HDAC8, HDAC4 and HDAC11, respectively. CS4 promotes α-tubulin and histone 3 acetylation. CS4 activates PPARγ and blocks glycolysis. CS4 induces cell cycle arrest at G2 phase and apoptosis, and shows anticancer effect both in vivo and in vitro .
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-
- HY-149912A
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|
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Polo-like Kinase (PLK)
Trk Receptor
Apoptosis
|
Cancer
|
|
CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 (PLK4) (IC50=2.6 nM). CZS-241 hydrochloride inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 hydrochloride induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 hydrochloride shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
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-
- HY-159517
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|
|
Apoptosis
PI3K
Akt
mTOR
STAT
|
Cancer
|
|
PI3K/Akt/mTOR-IN-5 (compound D3) is a derivative of Pseudolaric Acid B (HY-N6939) with anti-tumor activity. PI3K/Akt/mTOR-IN-5 inhibits excessive proliferation of tumor cells through the PI3K/AKT/mTOR and STAT3/GPX4 pathways. PI3K/Akt/mTOR-IN-5 effectively inhibits EDU positivity, reduces colony formation, places HCT-116 cells in the S phase and G2/M phase, and induces apoptosis .
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-
- HY-175261
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CDK
Wee1
Checkpoint Kinase (Chk)
|
Cancer
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|
DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies .
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-
- HY-10062
-
|
EBP-921
|
Akt
Farnesyl Transferase
|
Cancer
|
|
AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer .
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-
- HY-181606
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|
|
MDM-2/p53
Integrin
Apoptosis
|
Neurological Disease
Cancer
|
|
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is a dual MDM2 and α5β1 integrin modulator. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 acts as an antiproliferative agent, apoptosis inducer and cell cycle regulator, induces reactivation of p53 and upregulation of p21, redistributes glioblastoma cells from the G0/G1 phase to the G2/M phase, and enhances apoptosis. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is applicable to the research of glioblastoma .
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-
- HY-162319
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|
|
Apoptosis
HDAC
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity .
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-
- HY-155073
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
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-
- HY-161934
-
|
|
PARP
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
PARP1-IN-27 (Compound 9B) is the inhibitor for PARP1 and PARP2, with IC50 of 2.53 nM and 6.45 nM in cell SUM149PT. PARP1-IN-27 inhibits the proliferation of BRCA-mutated cancer cells SUM149PT, HCC1937 and Capan-1, with IC50 of 0.62, 1.91 and 4.26 μM respectively. PARP1-IN-27 aggravates DNA double-strand breaks, increases ROS generation, arrests cell cycle at G2/M phase, and induces apoptosis in SUM149PT .
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-
- HY-163511
-
|
|
Akt
Apoptosis
mTOR
PI3K
Microtubule/Tubulin
|
Cancer
|
|
PI3K/Akt/mTOR-IN-4 (compound 4r) is a potent PI3K/Akt/mTOR and tubulin polymerization inhibitor. PI3K/Akt/mTOR-IN-4 induce apoptosis and cell cycle arrest at G2/M phase. PI3K/Akt/mTOR-IN-4 decreases the expression of p-PI3K, p-Akt, and p-mTOR, β-tubulin .
|
-
- HY-P99712
-
|
hz208F2-4
|
IGF-1R
Apoptosis
ADC Antibody
|
Cancer
|
|
Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody, serveing as a targeting vector for antibody-drug conjugates (ADCs). Lonigutamab causes G2-M phase cell cycle arrest and increases apoptosis in IGF-1R-overexpressing tumor cells. Lonigutamab demonstrates potent antitumor efficacy in IGF-1R-overexpressing xenograft models. Lonigutamab can be used for the study of Solid tumors with overexpression of IGF-1R and thyroid eye
diseases .
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-
- HY-118522
-
|
|
Proteasome
NF-κB
Caspase
PARP
IAP
Apoptosis
|
Cancer
|
TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc .
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-
- HY-169096
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
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-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
|
-
- HY-178004
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-73 is a potent and selective VEGFR-2 inhibitor, showing selectively inhibition of VEGFR-2 (IC50 = 0.0787 μM) over EGFR (IC50 = 1.31 μM). VEGFR-2-IN-73 demonstrates potent antiproliferative activity across multiple cancer cell lines. VEGFR-2-IN-73 induces G2/M and Pre-G1 phase arrest and significantly enhances apoptosis. VEGFR-2-IN-73 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
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-
- HY-179018
-
|
|
Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
Topoisomerase II-IN-25 (Compound 6a) is a selective inhibitor of topoisomerase II and has no inhibitory activity on topoisomerase I. Topoisomerase II-IN-25 exhibits significant anti-PC-3 cell activity. Topoisomerase II-IN-25 significantly increases intracellular ROS levels, inducing oxidative stress. Topoisomerase II-IN-25 causes depolarization of mitochondrial membrane potential and promotes cell apoptosis. Topoisomerase II-IN-25 blocks PC-3 cells in the G2/M phase. Topoisomerase II-IN-25 can be used for the study of prostate cancer .
|
-
- HY-183787
-
|
|
PI3K
Akt
mTOR
Apoptosis
CDK
|
Cancer
|
|
PI3Kα-IN-33 is an orally active and selective PI3Kα inhibitor with an IC50 of 9.9 nM. PI3Kα-IN-33 blocks the PI3K/Akt/mTOR signaling pathway. PI3Kα-IN-33 induces apoptosis and triggers G2/M-phase arrest via Cyclin B1 and CDK1 downregulation. PI3Kα-IN-33 can be used for the research of colorectal cancer .
|
-
- HY-146253
-
|
|
CDK
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
|
-
- HY-180190
-
|
|
Microtubule/Tubulin
Bcl-2 Family
MDM-2/p53
CDK
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-85 (Compound C21) is a tubulin polymerization inhibitor (IC50 = 1.59 μM) targeting the colchicine binding site. Tubulin polymerization-IN-85 can cause cancer cells G2/M phase arrest and induce apoptosis. Tubulin polymerization-IN-85 downregulates the expression of Bcl-2, Bcl-xl, Mcl-1, Cyclin B1, cdc25, cdc2 protein and upregulates P53, P21, Bad and Bax levels. Tubulin polymerization-IN-85 can be used for the research of cancer, such as cervical cancer .
|
-
- HY-181074
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
|
Neurological Disease
Cancer
|
|
Tubulin polymerization-IN-88 is a tubulin inhibitor that blocks tubulin polymerization, leading to microtubule destabilization and disruption of the mitotic spindle. Tubulin polymerization-IN-88 induces G2/M phase arrest and apoptosis in cancer cells, and inhibits cancer cell migration and self-renewal of cancer stem cells. It exhibits in vitro anti-proliferative activity against cancer cells with selectivity over normal cells. Tubulin polymerization-IN-88 also demonstrates in vivo anti-cancer activity without significant toxicity. Tubulin polymerization-IN-88 is applicable for research on glioblastoma, lung cancer, endometrial cancer, ovarian cancer, and leukemia .
|
-
- HY-179399
-
|
|
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
β-carboline-ACS81 is a β-carboline derivative with potent antitumor properties. β-carboline-ACS81 induces apoptosis through the collapse of mitochondrial membrane potential and arrests cell cycle at G2/M phase in HL-60 cells. β-carboline-ACS81 possesses potent antiproliferative activity against HL-60 cells (IC50 = 1.52 μM). β-carboline-ACS81 can be used for the research of leukemia, histiocytic lymphoma, hepatocellular carcinoma, malignant melanoma, colorectal carcinoma and lung carcinoma .
|
-
- HY-175589
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
XSJ81 is an orally active anti-cancer agent. XSJ81 significantly inhibits the proliferation of ampullary carcinoma (AC) DPC-X3 cells with an IC50 of 0.655 μM. XSJ81 inhibits the colony formation, arrests cell cycle at the G2/M phase and inhibits the migration in DPC-X3 cells. XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. XSJ81 demonstrates significant anti-tumor efficacy in mice bearing DPC-X3 xenografts. XSJ81 can be used for the study of ampullary carcinoma .
|
-
- HY-173212
-
|
|
Polo-like Kinase (PLK)
c-Myc
Apoptosis
|
Cancer
|
|
PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC50: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-163747
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
|
-
- HY-179103
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK4-IN-5 (compound 5f) is a PLK4 (IC50 = 0.8 nM) inhibitor. PLK4-IN-5 can inhibit MCF-7 cell clone formation, induce cell cycle arrest (S/G2 phase), and apoptosis. PLK4-IN-5 has anti proliferative activity against MCF-7 cells (IC50 = 0.48 μM). PLK4-IN-5 can be used in the research of cancer such as breast cancer .
|
-
- HY-148712
-
|
|
Apoptosis
Sirtuin
|
Cancer
|
|
SIRT6 activator 12q is potent, selective and orally active SIRT6 activator with IC50 values of 171.20, >200, >200, >200, 0.58 μM for SIRT1, SIRT2, SIRT3, SIRT5, SIRT6, respectively. SIRT6 activator 12q inhibits cell growth and migration. SIRT6 activator 12q induces Apoptosis and cell cycle arrest at G2 phase. SIRT6 activator 12q shows anticancer activity .
|
-
- HY-N17440
-
|
|
Apoptosis
Caspase
Bcl-2 Family
DNA/RNA Synthesis
Bacterial
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
2-Methoxyjuglone, a naphthoquinone, is an apoptosis inducer. 2-Methoxyjuglone activates caspase-9 and caspase-3 via the mitochondrial cytochrome c-dependent intrinsic apoptosis cascade. 2-Methoxyjuglone increases pro-apoptotic Bax levels, decreases anti-apoptotic Bcl-2 levels, and promotes mitochondrial cytochrome c release. 2-Methoxyjuglone induces apoptosis morphological features, early apoptosis, S-phase and G2/M-phase cell cycle arrest, and DNA double-strand breaks. 2-Methoxyjuglone exerts activity against Gram-positive bacteria, pathogenic fungi, and phytopathogenic fungi. 2-Methoxyjuglone can be used for the research of hepatocellular carcinoma, osteosarcoma, colon adenocarcinoma, breast cancer, fungal infection, bacterial infection .
|
-
- HY-178989
-
|
|
Phosphoglycerate Kinase (PGK)
Cuproptosis
|
Cancer
|
|
PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma .
|
-
- HY-180809
-
|
|
PARP
|
Cancer
|
|
YCH3292, a derivative of YCH189 (HY-155993) is a potent, selective and orally active PARP1/2 inhibitor with IC50 both <0.001 nM. YCH3292 can increase the stability of PARP-DNA complexes. YCH3292 exhibits robust antiproliferative activity. YCH3292 can induce double-strand breaks in DNA, increase the protein levels of γH2AX, P-RPA32, and P-Chk1 and induce tumor cells S or G2/M phase arrest and apoptosis. YCH3292 can inhibit tumor growth in MC38 xenograft model .
|
-
- HY-178960
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-59 (Compound 8g) is an orally active Tubulin inhibitor. Tubulin-IN-59 exhibits potent anti-proliferative activity against HCT116 colorectal cancer, HeLa cervical cancer, and HepG2 liver cancer cell lines, with its IC₅₀ value ranging from 16 to 35 nM. Tubulin-IN-59 arrests HeLa cells in the G2/M phase and induces cell apoptosis. Tubulin-IN-59 demonstrates significant anti-tumor activity in the HT29 human colon cancer mouse xenograft model. Tubulin-IN-59 can be used for the study of colorectal cancer and cervical cancer .
|
-
- HY-181729
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
c-Myc
CDK
PARP
|
Cancer
|
|
PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer .
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-
- HY-13270A
-
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E7010 hydrochloride
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
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|
ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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-
- HY-182753
-
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Microtubule/Tubulin
P-glycoprotein
Apoptosis
CDK
Bcl-2 Family
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Cancer
|
|
Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine (HY-16569)-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer .
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- HY-160121
-
|
Patrinoside aglycone
|
Apoptosis
NO Synthase
TNF Receptor
Interleukin Related
PGE synthase
COX
|
Inflammation/Immunology
Cancer
|
|
Patrinoside aglucone (Compound 8) is an iridoid glucoside that can be isolated from the Valeriana tuberosa. Patrinoside aglucone has potent anticancer activity with G2/M phase tumor cell cycle arrest and apoptosis induction. Patrinoside aglucone also significantly inhibits the proliferation of cancer stem cells (such as MDA-MB-231 and U-251MG cells). Patrinoside aglucone has great anti-inflammatory activity by inhibiting NO release (IC50: 43.44 μM) and significantly reduces the level of TNF-α, IL-1β, IL-6, PGE2 and COX-2 .
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-
- HY-139604
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MARK
Apoptosis
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Cancer
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|
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
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-
- HY-121989
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|
(Z)-3,5,4'-Trimethoxystilbene
|
Microtubule/Tubulin
HCV
CDK
Akt
PAK
|
Infection
Metabolic Disease
Cancer
|
|
cis-Trismethoxy resveratrol ((Z)-3,5,4'-Trimethoxystilbene) is an anti-HCV agent and Tubulin inhibitor, with an IC50 of 4 μM against Tubulin. cis-Trismethoxy resveratrol induces G2/M phase cell cycle arrest, reduces DCLK1, decreases CDK1 levels, blocks phosphorylation of Akt Ser 473, and induces the expression of p21 Cip1/Waf1. cis-Trismethoxy resveratrol exhibits anti-tumor and hepatoprotective activities. cis-Trismethoxy resveratrol can be used in studies related to colon adenocarcinoma, hepatocellular carcinoma, hepatitis C, and liver injury .
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-
- HY-173619
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|
|
EGFR
|
Cancer
|
|
EGFR-IN-160 (Compound R12) is an EGFR inhibitor (IC50 values are 1.62, 0.49 and 0.98 μM for EGFR WT, EGFR T790M and EGFR L858R/T790M/C797S, respectively). EGFR-IN-160 induces G2/M and S phase arrest and apoptosis in NCI-H522 cells, and has anticancer activity. EGFR-IN-160 has antioxidant effects against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM) .
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- HY-181978
-
|
|
Ras
Apoptosis
MEK
ERK
CDK
|
Cancer
|
|
GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a KD of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer .
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- HY-176171
-
|
|
Microtubule/Tubulin
Hippo (MST)
YAP
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC50=0.36 μM; EC-109, IC50=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers .
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-
- HY-173039
-
|
|
Microtubule/Tubulin
Keap1-Nrf2
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
α-Tubulin polymerization-IN-1 (Compound 8l) is an inhibitor for α-Tubulin polymerization. α-Tubulin polymerization-IN-1 modulates the NRF2/KEAP-1 signaling pathway, induces ROS generation in PC-3 cell, thereby inducing apoptosis in PC-3. α-Tubulin polymerization-IN-1 inhibits the proliferation of PC-3 cell with a GI50 of 0.17 µM, arrests the cell cycle at G2/M phase. α-Tubulin polymerization-IN-1 exhibits antitumor efficacy in mouse model .
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-
- HY-168725
-
|
|
PROTACs
Kinesin
Apoptosis
|
Cancer
|
|
PROTAC KSP degrader 1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP degrader 1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP degrader 1 exhibits antitumor efficacy in mouse model . (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
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-
- HY-147858A
-
|
|
PROTACs
|
Cancer
|
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
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-
- HY-182382
-
|
|
Apoptosis
MDM-2/p53
Caspase
|
Cancer
|
|
Anticancer agent 311 is an apoptosis inducer and p53 modulator. Anticancer agent 311 increases p53 levels, activates cleaved caspase-3, reduces p-Cdc25C levels, and disrupts p-p44/42 MAPK phosphorylation. Anticancer agent 311 induces G2/M phase arrest, inhibits cancer cell viability in a concentration- and time-dependent manner, and exhibits low toxicity to non-cancer cells. Anticancer agent 311 prevents tumor growth and angiogenesis in mouse xenograft models without detectable toxicity. Anticancer agent 311 can be used for the research of lung cancer .
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-
- HY-143233
-
|
|
Pim
HDAC
Apoptosis
|
Cancer
|
|
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
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-
- HY-121605
-
|
|
Apoptosis
|
Cancer
|
|
RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
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-
- HY-147898
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research .
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-
- HY-178993
-
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PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3K/AKT-IN-5 (Compound 3h) is a PI3K/AKT inhibitor. PI3K/AKT-IN-5 exhibits outstanding broad-spectrum anti-cancer activity, especially being sensitive to colorectal cancer. PI3K/AKT-IN-5 significantly reduces cell colony formation, induces G2/M phase cell cycle arrest and cell apoptosis. PI3K/AKT-IN-5 can be used for research on colorectal cancer .
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-
- HY-147899
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|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-34 (Compound 6g) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-34 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-34 can be used in leukemia research .
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-
- HY-179044
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|
|
p38 MAPK
JNK
Caspase
Apoptosis
|
Cancer
|
|
MKK7-JNK activator 1 (Compound 10) is a MKK7-JNK pathway activator. MKK7-JNK activator 1 effectively inhibits the proliferation and migration of MDA-MB-468 cells, induces G2/M phase arrest and caspase -dependent apoptosis (independent of ROS production). MKK7-JNK activator 1 significantly increases the levels of p-MKK7 and p-JNK, but does not affect p-ERK or p-p38. MKK7-JNK activator 1 can be used for the study of triple-negative breast cancer (TNBC) .
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-
- HY-172256
-
|
|
PI4K
|
Cancer
|
|
PI4KIII beta inhibitor 5 is a PI4KIIIβ inhibitor with an IC50 of 19 nM. PI4KIII beta inhibitor 5 can induce cancer cell apoptosis (Apoptosis), cell cycle arrest at the G2/M phase, and autophagy (Autophagy) by inhibiting the PI3K/AKT pathway. PI4KIII beta inhibitor 5 has also demonstrated significant antitumor activity in the H446 xenograft model of small cell lung cancer. PI4KIII beta inhibitor 5 can be used for research in the field of cancer therapy .
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-
- HY-147900
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-35 (Compound 6l) is a highly selective PI3K inhibitor with IC50 values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research .
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-
- HY-N1988R
-
|
Hemslecin A (Standard)
|
Reference Standards
Apoptosis
EGFR
Autophagy
MEK
Caspase
ERK
STAT
Survivin
Raf
p38 MAPK
CaMK
|
Inflammation/Immunology
Cancer
|
|
Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
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-
- HY-175713
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin/CDC5L-IN-1 is a Tubulin/CDC5L dual inhibitor. Tubulin/CDC5L-IN-1 targets to CDCL5 with a KD of 103.7 μM. Tubulin/CDC5L-IN-1 can inhibit multiple cancer cell proliferation and induce G2/M phase arrest. Tubulin/CDC5L-IN-1 induce cell apoptosis and ROS production. Tubulin/CDC5L-IN-1 exhibits antiangiogenic effects. Tubulin/CDC5L-IN-1 can be used for the research of cancer, such as colon carcinoma .
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-
- HY-178441
-
|
|
Pyruvate Kinase
Reactive Oxygen Species (ROS)
Apoptosis
Microtubule/Tubulin
|
Metabolic Disease
Cancer
|
|
PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer .
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-
- HY-161826
-
|
|
Wnt
β-catenin
HSP
CDK
c-Myc
|
Cancer
|
|
Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
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-
- HY-175021
-
|
|
HDAC
Carbonic Anhydrase
Microtubule/Tubulin
PARP
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
HDAC-IN-91 is a multiple inhibitor of HDAC (IC50 = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (Ki = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC50 = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research .
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-
- HY-165503
-
|
|
Wnt
β-catenin
|
Cancer
|
|
AZ1366 is an orally active tankyrase inhibitor. AZ1366 stabilizes Axin2, reduces NuMA levels, disrupts the interaction between tankyrase and NuMA, induces G2/M phase arrest, inhibits the Wnt pathway, and downregulates the expression of β-catenin-dependent genes. AZ1366 inhibits tumor growth in colorectal cancer xenograft models. AZ1366 synergistically inhibits the proliferation of non-small cell lung cancer cells, improves tumor control and significantly prolongs survival in orthotopic non-small cell lung cancer mouse models. AZ1366 is applicable to research related to colorectal cancer and non-small cell lung cancer .
|
-
- HY-178432
-
|
|
SHMT
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 (SHMT2) inhibitor with an IC50 of 1.21 μM and a KD of 10.6 μM. SHMT2-IN-1 binds to the folate binding site of SHMT2. SHMT2-IN-1 also inhibits SHMT1 with an IC50 of 1.83 μM. SHMT2-IN-1 can inhibit cancer cells proliferation, migration and invasion. SHMT2-IN-1 can induce cells apoptosis and ROS production and cause G2/M phase arrest. SHMT2-IN-1 can be used for the research of cancer, such as esophageal cancer .
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-
- HY-116504
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
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-
- HY-182752
-
|
|
CDK
Aurora Kinase
Apoptosis
|
Cancer
|
|
CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC50 of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer .
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-
- HY-175874
-
|
|
Microtubule/Tubulin
PI3K
Akt
Apoptosis
|
Cancer
|
|
Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer .
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-
- HY-168714
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 12 (Compound 2k) is an inhibitor for microtubule polymerization with an IC50 of 22.23 μM. Microtubule inhibitor 12 arrests the cell cycle of B16-F10 at G2/M phase, induces apoptosis in B16-F10, and inhibits cell migration. Microtubule inhibitor 12 inhibits the proliferation of cancer cells B16-f10, A549, HepG2 and MCF-7, with IC50s of 0.098, 0.135, 0.109, and 0.259 μM, respectively. Microtubule inhibitor 12 exhibits antitumor efficacy in mouse model .
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-
- HY-178939
-
|
|
EGFR
Akt
PERK
Apoptosis
|
Neurological Disease
Cancer
|
|
EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases .
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-
- HY-155523
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
|
Cancer
|
|
Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
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-
- HY-181528
-
|
|
JAK
CDK
|
Cancer
|
|
JAK1/CDK7-IN-1 (compound 11) is a JAK1/CDK7 inhibitor and cytotoxic agent.JAK1/CDK7-IN-1 forms a stable, tightly bound complex with JAK1.JAK1/CDK7-IN-1 disrupts cell cycle, induces G2/M phase arrest, and increases Pre-G1 phase cell proportion.JAK1/CDK7-IN-1 induces apoptosis, elevates caspase 1, 3, and 9 levels, and triggers apoptotic and necrotic cell death.JAK1/CDK7-IN-1 can be used for the research of breast cancer, prostate cancer .
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-
- HY-178343
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
|
-
- HY-175700
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved
caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC) .
|
-
- HY-178472
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
|
-
- HY-173481
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-37 (Compound 24) is a CDK9 inhibitor (EC50: 5.5 nM) with weak inhibition on other CDK isoforms, showing high selectivity. CDK9-IN-37 has significant antiproliferative activity against acute myeloid leukemia MOLM-13 cells (IC50: 0.034 μM). CDK9-IN-37 inhibits the CDK9 signaling pathway, reduces the phosphorylation level of RNAP II CTD (Ser2), downregulates the anti-apoptotic protein McI-1, induces cell apoptosis, and arrests the cell cycle at the G2/M phase. CDK9-IN-37 can be used in the study of acute myeloid leukemia (AML) .
|
-
- HY-170927
-
|
|
JAK
STAT
Apoptosis
|
Cancer
|
|
JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC50s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI50 of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .
|
-
- HY-15898
-
Y-320
5 Publications Verification
|
Interleukin Related
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Y-320 is a potent, orally active phenylpyrazoleanilide immunomodulator. Y-320 inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM. Y-320 enhances TP53, DMD, and COL17A1 PTC readthrough by G418 and increases cellular protein levels and protein synthesis. Y-320 concomitants use of with a low dose of Paclitaxel (HY-B0015) significantly sensitized multidrug resistance (MDR) tumors by inducing G2/M phase arrest and apoptosis. Y-320 can be used for research of rheumatoid arthritis (RA) and cancer .
|
-
- HY-172217
-
|
|
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC50 of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC50s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .
|
-
- HY-N0712
-
|
|
Autophagy
mTOR
Akt
FXR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Typhaneoside is an orally bioavailable signal modulator and cellular regulator. Typhaneoside regulates the PI3K/Akt/mTOR autophagy transduction pathway. Typhaneoside promotes the activation of AMP-activated protein kinase and Caspase-3, induces apoptosis, ferroptosis, autophagy, ROS accumulation, and cell cycle arrest at the G2/M phase, and reduces cancer cell viability. Typhaneoside activates the farnesoid X receptor signaling pathway, improves glucose and lipid metabolism, alleviates inflammatory responses, oxidative stress and hepatic lipid accumulation, and exerts hepatoprotective effects. Typhaneoside is applicable to research related to post-myocardial infarction heart failure, acute myeloid leukemia, non-alcoholic fatty liver disease, and neurological disorders .
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-
- HY-168574
-
|
|
PROTACs
Sirtuin
Apoptosis
|
Cancer
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SZU-B6 is a PROTAC degrader for SIRT6 with DC50 of 45 nM and 154 nM in cell SK-HEP-1 and Huh-7. SZU-B6 inhibits the proliferation of cell SK-HEP-1 with an IC50 of 1.51 μM, inhibits the colony formation of SK-HEP-1 and Huh-7, induces apoptosis and arrests the cell cycle at G2/M phase in SK-HEP-1. SZU-B6 exhibits antitumor efficacy in mouse model. (Pink: ligand for target protein (HY-16605); Black: linker (HY-W012935); BLue: ligand for E3 ligase (HY-W453548)
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- HY-134061
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Apoptosis
Mitosis
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Cancer
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Arecaidine propargyl ester hydrobromide is an agonist of M2 muscarinic acetylcholine receptors and has the activity of inhibiting tumor cell proliferation. The application of arecaidine propargyl ester hydrobromide has shown that it can reduce the number of ovarian cancer cells in vitro and induce apoptosis and the production of reactive oxygen species (ROS) at specific concentrations. Arecaidine propargyl ester hydrobromide can also arrest cells at the G2/M phase of the cell cycle and increase the percentage of abnormal mitosis. Arecaidine propargyl ester hydrobromide is more sensitizing to ovarian surface epithelial cells with higher M2 receptor levels than to cancer cells. Arecaidine propargyl ester hydrobromide exhibits the effect of lowering arterial blood pressure when interacting with the cardiovascular system in a natural physiological state, indicating its potential pharmacological application .
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- HY-173331
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Chloride Channel
Apoptosis
Autophagy
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Cancer
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Antitumor agent-201 (Compound 10) is a chloride transport activator that targets the Golgi apparatus. Its EC50 for promoting the transmembrane transport of chloride ions is 1.53 mol%, and its IC50 against HepG2 cells is 7.13 μM. Antitumor agent-201 exerts its anti-cancer activity by selectively acting on the Golgi apparatus, disrupting the chloride ion homeostasis within it, reducing the expression of key proteins such as GM130 and GRASP55, altering the structure and function of the Golgi apparatus, triggering Autophagy of the Golgi apparatus, and further inducing Apoptosis of cancer cells and arresting cancer cells in the G2/M phase. Antitumor agent-201 can be used in the research field of cancer diseases .
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- HY-13270R
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E7010 (Standard)
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Microtubule/Tubulin
Autophagy
Apoptosis
Reference Standards
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Cancer
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ABT-751 (Standard) is the analytical standard of ABT-751. This product is intended for research and analytical applications. ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
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- HY-168895
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AP-1
ERK
Apoptosis
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Cancer
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c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth .
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- HY-180124
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CDK
Wnt
β-catenin
c-Myc
Reactive Oxygen Species (ROS)
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Cancer
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CDK8-IN-20 (Compound 67j) is a selective, potent and orally active type I CDK8 inhibitor with an IC50 of 70.5 nM. CDK8-IN-20 shows IC50 values of 147.8, 726.9 and 217.4 nM for homologous kinase CDK19, CDK7 and CDK9. CDK8-IN-20 can inhibit the Wnt/β-catenin pathway and downregulate the expression of β-catenin, Cyclin D1, and c-Myc. CDK8-IN-20 can induce ROS production and cause G2/M and S phase arrest. CDK8-IN-20can be used for the research of cancer, such as colon cancer .
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- HY-182372
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Epoxide Hydrolase
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Neurological Disease
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SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
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- HY-182245
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Microtubule/Tubulin
Carbonic Anhydrase
Apoptosis
MDM-2/p53
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Cancer
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Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
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- HY-180820
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Drug Derivative
MDM-2/p53
CDK
Reactive Oxygen Species (ROS)
Apoptosis
Bcl-2 Family
Caspase
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Cancer
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Dimethyl bisphenolate (Compound DMB) is a natural neolignan derivative with orally active anti-tumor activity. Dimethyl bisphenolate can inhibit cancer cells proliferation, invasion and migration. Dimethyl bisphenolate can activate the p53 signaling pathway, upregulate the expression of p21 protein, inhibit the activity of the CDK1-cyclin B1 complex, and cause cells to stall at the G2/M phase. Dimethyl bisphenolate can induce ROS production, upregulate pro-apoptotic proteins Noxa and Bim, downregulate anti-apoptotic protein Bcl-2, activate caspase-9 and caspase-3, and ultimately induce cell apoptosis. Dimethyl bisphenolate can be used for research of glioblastoma .
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- HY-147825
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EGFR
Raf
Apoptosis
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Cancer
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EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
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- HY-170965
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CDK
DNA/RNA Synthesis
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Cancer
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Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
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- HY-N0440
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Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
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Infection
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity .
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- HY-161863
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Microtubule/Tubulin
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
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- HY-15558
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bisBenzimide H 33258; H 33258
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Fluorescent Dye
DNA Stain
DNA Alkylator/Crosslinker
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Others
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Hoechst 33258 is a blue to blue-green fluorescent live cell dye that can label DNA. Hoechst 33258 can specifically bind to the minor groove of DNA (and tends to bind to A/T-rich DNA), resulting in a significant increase in fluorescence intensity. Hoechst 33258 can cross the cell membrane and cause changes in DNA structure, such as G2/M phase arrest. Hoechst 33258 can bind to live or fixed cells, and the fluorescence intensity increases with increasing solution pH. As a DNA-specific probe, Hoechst 33258 can be used to detect DNA content, analyze cell cycle, etc. The excitation wavelength of Hoechst 33258 is 350-365 nm, and the emission wavelength is 460-490 nm .
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- HY-124309
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Lactate Dehydrogenase
Apoptosis
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Cancer
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NHI-2 is a lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 14.7 µM. NHI-2 shows selective for LDHA over LDHB (IC50 = 55.8 µM). NHI-2 is an efficient anti-glycolytic agent. NHI-2 enhances apoptosis, induces cell cycle arrest at S and G2 phases. NHI-2 has a broad spectrum anti-proliferative activity in cancer cells. NHI-2 affects extracellular acidification rate and ATP production. NHI-2 suppresses tumor growth in murine B78 melanoma tumor model .
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- HY-126251
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CDK
Apoptosis
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Cancer
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CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC .
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- HY-183373
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EGFR
PARP
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Cancer
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EGFR/PARP-1-IN-1 is a dual EGFR and PARP-1 inhibitor with IC50 values of 64 nM and 12 nM, respectively. EGFR/PARP-1-IN-1 binds to the ATP-binding pocket of EGFR and interacts with the catalytic domain of PARP-1, inhibiting kinase and enzymatic activity via hydrogen bond formation with key residues in both targets. EGFR/PARP-1-IN-1 induces apoptosis through the endogenous mitochondrial pathway, arrests the cell cycle at the G2 phase, and inhibits cell proliferation. EGFR/PARP-1-IN-1 can be used for research on triple-negative breast cancer .
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- HY-182795
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MMP
Interleukin Related
TGF-beta/Smad
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Metabolic Disease
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Colchicine derivative-1 is a colchicine derivative. Colchicine derivative-1 exhibits cytotoxicity against various cells. Colchicine derivative-1 arrests cancer cells at the G2/M phase of the cell cycle. Colchicine derivative-1 increases the levels of MMP-2, MMP-8, MMP-9, IL-2, IL-6, IL-17A, IL-22, IL-4, and IL-5 in the blood, inhibits the gene expression of hepatic fibrinogen α, β, γ and TGF-β1, and alleviates hepatic fibrosis symptoms in mice. Colchicine derivative-1 has antifibrotic activity and can be used in studies related to hepatic fibrosis .
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- HY-121605S
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Isotope-Labeled Compounds
Apoptosis
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Cancer
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RL71-d6 is a deuterium labeled RL71 (HY-121605). RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
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- HY-169938
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HDAC
Histone Demethylase
Apoptosis
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Cancer
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LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
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- HY-174428
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PROTACs
JAK
STAT
Apoptosis
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Cancer
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PROTAC JAK2 degrader-1 is a JAK2 PROTAC degrader, with a DC50 of 27.35 nM. PROTAC JAK2 degrader-1 induces JAK2 degradation via the ubiquitin-proteasome pathway. PROTAC JAK2 degrader-1 inhibits the JAK2-STAT signaling pathway. PROTAC JAK2 degrader-1 induces G2/M phase arrest and apoptosis in cancer cells. PROTAC JAK2 degrader-1 exhibits antiproliferative activity against cancer cells. PROTAC JAK2 degrader-1 inhibits recombinant human erythropoietin (rhEPO)-mediated polycythemia and splenomegaly in mice. PROTAC JAK2 degrader-1 can be used for research on myeloproliferative neoplasms, including polycythemia vera .
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- HY-172158
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Anaplastic lymphoma kinase (ALK)
Caspase
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Cancer
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ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m 6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia .
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- HY-N2374
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Apoptosis
NF-κB
MMP
Adrenergic Receptor
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Inflammation/Immunology
Cancer
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Eupatorin is an orally active flavonoid with antiproliferative and vasodilatory properties. Eupatorin downregulates the expression levels of NF-κB, MMP9, IL-1β and TNF-α. Eupatorin induces apoptosis, G2/M phase cell cycle arrest, and reactive oxygen species (ROS) production. Eupatorin modulates the activities of muscarinic receptors and β-adrenergic receptors; inhibits sarcoplasmic reticulum calcium release and calcium channels; and activates the NO/sGC/cGMP pathway, indomethacin-sensitive pathway, and potassium channel pathway. Eupatorin exerts cytotoxic effects on cancer cell lines, and is metabolized by CYP1A1 and CYP1 family enzymes to form metabolites with antiproliferative activity. Eupatorin can be used in research related to breast cancer, hypertension, and leukemia .
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- HY-170451
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KT-253
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PROTACs
MDM-2/p53
Apoptosis
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Cancer
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Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)) .
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- HY-181061
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COX
EGFR
Lipoxygenase
FAK
Raf
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC50 of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer .
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- HY-146095
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MDM-2/p53
DNA/RNA Synthesis
Apoptosis
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Cancer
|
|
p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
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- HY-168437
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|
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MicroRNA
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Cancer
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LIN28-IN-2 is a Lin28 inhibitor with activity against Lin28a, Lin28b, and their zinc knuckle domain. LIN28-IN-2 blocks Lin28-RNA substrate binding, perturbs zinc knuckle domain conformation. LIN28-IN-2 inhibits cancer cell proliferation, spheroid growth, and induces G2/M phase arrest. LIN28-IN-2 suppresses cancer stem cell phenotypes, Lin28-mediated stress granule formation, let-7 target genes, cancer stem cell biomarkers, and neuroendocrine biomarkers expression in cancer cells. LIN28-IN-2 can be used for the research of cancer .
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- HY-147858
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PROTACs
EGFR
Apoptosis
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Cancer
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-170924
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Microtubule/Tubulin
Apoptosis
Mitosis
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Cancer
|
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Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active Tubulin polymerization inhibitor. Tubulin polymerization-IN-76 inhibits Tubulin polymerization with an IC50 of 2.505 μM by acting on the colchicine binding site, thereby disrupting intracellular Microtubule networks and interfering with cell mitosis. Tubulin polymerization-IN-76 demonstrates exceptional efficacy against MGC-803 and HGC-27 cells with IC50s of 1.61 and 1.82 nM, respectively. Tubulin polymerization-IN-76 effectively inhibits the colony formation and cell migration activities, and induces G2/M phase cycle arrest and Apoptosis in MGC-803 and HGC-27 cells.Tubulin polymerization-IN-76 shows a broad-spectrum antiproliferative activity .
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- HY-N16771
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Caspase
Apoptosis
Bcl-2 Family
Bacterial
VEGFR
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Cancer
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Clausenidin is a selective inhibitor targeting apoptosis-related pathways, including the mitochondrial pathway and death receptor pathway, and vascular endothelial growth factor (VEGF). Clausenidin induces mitochondrial membrane depolarization by activating caspase-3, caspase-8 and caspase-9, upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-2. Clausenidin also inhibits VEGF expression and blocks angiogenesis, exerting anti-tumor activity. Clausenidin has inhibitory effects against Mycobacterium tuberculosis (MIC=200 μg/mL). Clausenidin can induce apoptosis in liver cancer cells, arrest the cell cycle in the G2/M phase, and inhibit tumor angiogenesis. Clausenidin can be used in the research of malignant tumors such as liver cancer .
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- HY-161688
-
|
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Apoptosis
HDAC
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Cancer
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|
HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
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- HY-163099
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Drug-Linker Conjugates for ADC
Topoisomerase
Apoptosis
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Cancer
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P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
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- HY-114214
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Drug Derivative
NF-κB
MMP
TNF Receptor
Interleukin Related
Cyclin G-associated Kinase (GAK)
CDK
PI3K
Akt
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Inflammation/Immunology
Cancer
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CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway . CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway . CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells . CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer .
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- HY-169067
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Mtx-C
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DNA/RNA Synthesis
p38 MAPK
Bacterial
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Infection
Cancer
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10-Methoxy-canthin-6-one (Mtx-C) is analkaloid derivative. 10-Methoxy-canthin-6-one can induce DNA damage by intercalating into DNA. 10-Methoxy-canthin-6-one can inhibit cancer cells proliferation, cause G2/M phase arrest and induce myeloid differentiation. T10-Methoxy-canthin-6-one can upregulate the expression of myeloperoxidase, CD15, CD11b, and CD14, as well as activation of p38 MAPK. 10-Methoxy-canthin-6-one also exhibits anti-bacterial activity. 10-Methoxy-canthin-6-one can be used for the researches of cancer and infection, such as acute myeloid leukemias (AML) .
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- HY-181502
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EGFR
ERK
PARP
Caspase
Bcl-2 Family
Apoptosis
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Cancer
|
|
EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFR L858R/T790M and EGFR L858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC) .
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-
- HY-182281
-
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FLT3
STAT
Akt
ERK
Apoptosis
|
Cancer
|
|
FLT3-IN-41 is a highly potent FLT3 inhibitor. The IC50 values of FLT3-IN-41 against human FLT3-ITD and FLT3-WT are 3.16 nM and 294.7 nM, respectively. By binding to the ATP-binding pockets of FLT3-ITD and FLT3-WT and forming hydrogen bonds with hinge region residues and Phe830, FLT3-IN-41 inhibits the STAT5, Akt and Erk signaling pathways. FLT3-IN-41 induces G2/M phase arrest and promotes apoptosis in FLT3-ITD-positive acute myeloid leukemia cells, exhibiting significant antiproliferative activity. FLT3-IN-41 serves as a valuable tool for the study of acute myeloid leukemia .
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-
- HY-12708
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Chlorpromazine
Maximum Cited Publications
128 Publications Verification
|
Dopamine Receptor
Cytochrome P450
Autophagy
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
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Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
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- HY-120339
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|
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Microtubule/Tubulin
FAK
MEK
ERK
MMP
Caspase
PARP
Apoptosis
MDM-2/p53
|
Cancer
|
|
STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC50 values ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers .
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-
- HY-170329
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|
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PROTACs
Androgen Receptor
Apoptosis
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Cancer
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PROTAC AR Degrader-8 is the PROTAC degrader for androgen receptor (AR) that degrades AR-FL with DC50s of 0.018 μM and 0.14 μM in 22Rv1 cell and LNCaP cell, degrades AR-V7 with DC50 of 0.026 μM in 22Rv1 cell. PROTAC AR Degrader-8 inhibits the proliferation of cancer cell 22Rv1 and LNCaP with IC50 values of 0.038 μM and 1.11 μM. PROTAC AR Degrader-8 arrests cell cycle at G2/M phase, induces apoptosis in 22Rv1 cell. PROTAC AR Degrader-8 exhibits anticancer efficacy in mouse and zebrafish model. PROTAC AR Degrader-8 can be used for the research of prostate cancer, castration-resistant prostate cancer .
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- HY-179372
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50 = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.
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- HY-N3001
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STAT
VEGFR
Bcl-2 Family
Survivin
IAP
NF-κB
Apoptosis
Caspase
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Neurological Disease
Inflammation/Immunology
Cancer
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Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury .
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- HY-N11846
-
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Apoptosis
Caspase
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Inflammation/Immunology
Cancer
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4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases .
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- HY-B0407A
-
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Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
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Cardiovascular Disease
Neurological Disease
Cancer
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Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
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- HY-B0407AR
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Reference Standards
Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
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|
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
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- HY-162098
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PROTACs
Microtubule/Tubulin
Apoptosis
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Cancer
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PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
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- HY-N0440R
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|
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Reference Standards
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity .
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- HY-N10342
-
|
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Apoptosis
Bcl-2 Family
Caspase
PARP
Reactive Oxygen Species (ROS)
Bacterial
PI3K
Akt
NF-κB
P-glycoprotein
|
Infection
Cancer
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Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp. . Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections .
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- HY-N3000
-
|
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JNK
IRE1
Akt
mTOR
YAP
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Fungal
|
Infection
Inflammation/Immunology
Cancer
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6-Methoxydihydrosanguinarine is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .
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- HY-181673
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|
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Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
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ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma .
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-
- HY-W041470R
-
|
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
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-
- HY-N3000A
-
|
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JNK
IRE1
Akt
mTOR
YAP
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Fungal
Caspase
DNA/RNA Synthesis
|
Infection
Inflammation/Immunology
Cancer
|
|
6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .
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-
- HY-174870
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|
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PROTACs
Estrogen Receptor/ERR
Apoptosis
Fluorescent Dye
|
Cancer
|
|
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
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-
- HY-175298
-
|
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STAT
Src
Apoptosis
|
Cancer
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STAT-3/c-Src-IN-1 (Compound 12d) is a dual STAT-3 (IC50=0.844 μM) and c-Src (IC50=0.268 μM) inhibitor. STAT-3/c-Src-IN-1 blocks tumor cell proliferation, migration, and angiogenesis signaling pathways. STAT-3/c-Src-IN-1 exhibits potent anti-proliferative activity against melanoma (SK-MEL-2) and CNS cancer (SNB-75) cell lines (GI50=-5.75 μM and -5.63 μM), inducing tumor cell apoptosis via G0/G1 and G2/M phase cell cycle arrest. STAT-3/c-Src-IN-1 is promising for research of melanoma and glioblastoma .
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- HY-178032
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PARP
Apoptosis
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
STING
|
Cancer
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|
PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC50 = 0.6 nM), and also inhibits PARP2 (IC50 = 1.0 nM) and PARP7 (IC50 = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .
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-
- HY-182745
-
|
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VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-85 is a strong VEGFR-2 inhibitor, with an IC50 value of 0.23 μM. VEGFR-2-IN-85 exhibits potent cytotoxic activity against multiple cancer cell lines with minimal toxicity toward normal cells. VEGFR-2-IN-85 also impairs cancer cell migration, likely through modulation of the VEGFR-2/p-Akt pathway. VEGFR-2-IN-85 can induce apoptosis through modulation of Caspase-3, Bax and Bcl-2. VEGFR-2-IN-85 arrests cell cycle at the G2/M phase and has anti-angiogenic activity. VEGFR-2-IN-85 is a targeted radiosensitizer enhancing radiation-induced cytotoxicity. VEGFR-2-IN-85 can be used for research on cancers such as non-small cell lung cancer, breast cancer, and liver cancer .
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-
- HY-179049
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|
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EGFR
Microtubule/Tubulin
Akt
ERK
Autophagy
Atg8/LC3
p62
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
EGFR/tubulin-IN-1 (Compound 26) is a dual-target inhibitor of EGFR and tubulin. EGFR/tubulin-IN-1 significantly reduces the levels of p-EGFR, p-AKT, and p-ERK in cells, disrupting the microtubule structure of the cells. EGFR/tubulin-IN-1 significantly inhibits the proliferation of H1975 cells and significantly blocks the cells in the G2/M phase. EGFR/tubulin-IN-1 induces the expression of autophagy markers LC3B-II and Beclin-1, while down-regulating the expression of p62. EGFR/tubulin-IN-1 induces ferroptosis, with increased ROS content and depletion of glutathione (GSH). EGFR/tubulin-IN-1 inhibits epithelial-mesenchymal transition (EMT) and tumor metastasis. EGFR/tubulin-IN-1 has a significant tumor-suppressing effect in the H1975 transplanted tumor nude mouse model. EGFR/tubulin-IN-1 can be used for the study of non-small cell lung cancer .
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-
- HY-172891
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|
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CDK
HDAC
Apoptosis
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Cancer
|
|
CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17 μM, 1.73 μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer .
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-
- HY-125942
-
|
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CRAC Channel
TRP Channel
CaMK
Akt
Apoptosis
Autophagy
Na+/Ca2+ Exchanger
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
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-
- HY-N0430
-
|
Coptisin
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
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-
- HY-N5112A
-
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Arnebin 1
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
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Inflammation/Immunology
|
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β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
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-
- HY-100001
-
|
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TRP Channel
CRAC Channel
Autophagy
CaMK
Akt
Apoptosis
Na+/Ca2+ Exchanger
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
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- HY-N0430A
-
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Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
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-
- HY-144292
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HDAC
|
Cancer
|
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HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy .
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- HY-N1039A
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Others
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Cancer
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Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle .
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-
- HY-115452
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JAK
Apoptosis
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Cancer
|
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study .
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-
- HY-130326
-
|
Ru(η6-p-cymene)Cl2(pta)
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Apoptosis
Caspase
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Cardiovascular Disease
Cancer
|
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RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model .
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| Cat. No. |
Product Name |
Type |
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- HY-15558
-
|
bisBenzimide H 33258; H 33258
|
Fluorescent Dye
|
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Hoechst 33258 is a blue to blue-green fluorescent live cell dye that can label DNA. Hoechst 33258 can specifically bind to the minor groove of DNA (and tends to bind to A/T-rich DNA), resulting in a significant increase in fluorescence intensity. Hoechst 33258 can cross the cell membrane and cause changes in DNA structure, such as G2/M phase arrest. Hoechst 33258 can bind to live or fixed cells, and the fluorescence intensity increases with increasing solution pH. As a DNA-specific probe, Hoechst 33258 can be used to detect DNA content, analyze cell cycle, etc. The excitation wavelength of Hoechst 33258 is 350-365 nm, and the emission wavelength is 460-490 nm .
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- HY-W127705
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|
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Fluorescent Dye
|
|
Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes .
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- HY-15149G
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FK 228; FR 901228; NSC 630176
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Fluorescent Dye
|
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Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
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| Cat. No. |
Product Name |
Type |
-
- HY-B2201
-
|
Sodium citrate; Trisodium citrate anhydrous
|
Biochemical Assay Reagents
|
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Citric acid trisodium (Sodium citrate) is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-N1428A
-
|
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Biochemical Assay Reagents
|
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Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-B1295
-
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Litarex tetrahydrate
|
Biochemical Assay Reagents
|
|
Lithium citrate (Litarex) tetrahydrate is a natural preservative and food tartness enhancer. Lithium citrate tetrahydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Lithium citrate tetrahydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Lithium citrate tetrahydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-N1428CA
-
|
|
Biochemical Assay Reagents
|
|
Ferric citrate, suitable for cell culture is a natural preservative and food tartness enhancer. Ferric citrate, suitable for cell culture induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Ferric citrate, suitable for cell culture causes oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Ferric citrate, suitable for cell culture is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-W008606
-
|
Citric acid monosodium salt
|
Biochemical Assay Reagents
|
|
Sodium citrate monobasic (Citric acid monosodium salt) is a natural preservative and food tartness enhancer. Sodium citrate monobasic induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Sodium citrate monobasic cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Sodium citrate monobasic is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-W127841
-
|
|
Biochemical Assay Reagents
|
|
Citric acid-2,4- 13C2 is the 13C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-15149G
-
|
FK 228; FR 901228; NSC 630176
|
Biochemical Assay Reagents
|
|
Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
|
-
- HY-N1428AR
-
|
|
Biochemical Assay Reagents
|
|
Citric acid monohydrate (Standard) is the analytical standard of Citric acid monohydrate (HY-N1428A). This product is intended for research and analytical applications. Citric acid monohydrate is a natural preservative and food tartness enhancer. Citric acid monohydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid monohydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid monohydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
- HY-B1295R
-
|
Litarex tetrahydrate (Standard)
|
Biochemical Assay Reagents
|
|
Lithium citrate (tetrahydrate) (Standard) is the analytical standard of Lithium citrate (tetrahydrate). This product is intended for research and analytical applications. Lithium citrate (Litarex) tetrahydrate is a natural preservative and food tartness enhancer. Lithium citrate tetrahydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Lithium citrate tetrahydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Lithium citrate tetrahydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-16375
-
|
D-63153
|
GnRH Receptor
Apoptosis
|
Cancer
|
|
Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer .
|
-
- HY-144292
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). HDAC-IN-30 exhibits potent antitumor efficacy .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991501
-
|
HcHAb18
|
ADC Antibody
Transmembrane Glycoprotein
SARS-CoV
|
Infection
Cancer
|
|
Meplazumab (HcHAb18) is a humanized anti-CD147 IgG1 antibody a Kd of 0.47 nM. Meplazumab shows anti-SARS-CoV-2 and antitumor activity. Meplazumab conjugated with DM1 can form an antibody-conjugated drug ( HcHAb18-DM1), which induces G2/M phase cell cycle arrest and exerts antiproliferative activity in cancer cells. Meplazumab can be used for the researches of COVID-19 pneumonia and non-small cell lung cancer .
|
-
(5)
-
- HY-P99662
-
|
MLN0264; TAK-264
|
Antibody-Drug Conjugates (ADCs)
Guanylate Cyclase
Apoptosis
|
Cancer
|
|
Indusatumab vedotin (MLN-0264; AKT-264) is an antibody-drug conjugate (ADC) consisting of the human anti-guanylate cyclase C (GCC) antibody linked to a microtubule-disruptor Monomethyl auristatin (HY-15162). Indusatumab vedotin has anti-proliferative effects on pancreas cancer cell lines. Indusatumab vedotin arrests cell cycle at G2/M phase, and induces apoptosis .
|
-
(5)
-
- HY-P99712
-
|
hz208F2-4
|
IGF-1R
Apoptosis
ADC Antibody
|
Cancer
|
|
Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody, serveing as a targeting vector for antibody-drug conjugates (ADCs). Lonigutamab causes G2-M phase cell cycle arrest and increases apoptosis in IGF-1R-overexpressing tumor cells. Lonigutamab demonstrates potent antitumor efficacy in IGF-1R-overexpressing xenograft models. Lonigutamab can be used for the study of Solid tumors with overexpression of IGF-1R and thyroid eye
diseases .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1428
-
-
-
- HY-B1357
-
-
-
- HY-N0168
-
-
-
- HY-N6722
-
-
-
- HY-N0047
-
-
-
- HY-N0421
-
-
-
- HY-W009156
-
-
-
- HY-N1988
-
-
-
- HY-N0712
-
|
|
Cardiovascular Disease
Flavonols
Structural Classification
Flavonoids
Typhaceae
Classification of Application Fields
Typha angustifolia L.
Phenols
Polyphenols
Plants
Disease Research Fields
Source Classification
|
Autophagy
mTOR
Akt
FXR
|
|
Typhaneoside is an orally bioavailable signal modulator and cellular regulator. Typhaneoside regulates the PI3K/Akt/mTOR autophagy transduction pathway. Typhaneoside promotes the activation of AMP-activated protein kinase and Caspase-3, induces apoptosis, ferroptosis, autophagy, ROS accumulation, and cell cycle arrest at the G2/M phase, and reduces cancer cell viability. Typhaneoside activates the farnesoid X receptor signaling pathway, improves glucose and lipid metabolism, alleviates inflammatory responses, oxidative stress and hepatic lipid accumulation, and exerts hepatoprotective effects. Typhaneoside is applicable to research related to post-myocardial infarction heart failure, acute myeloid leukemia, non-alcoholic fatty liver disease, and neurological disorders .
|
-
-
- HY-B1295
-
-
-
- HY-N2983
-
-
-
- HY-N4327
-
-
-
- HY-N0440
-
-
-
- HY-N2374
-
-
-
- HY-N5112A
-
|
Arnebin 1
|
Quinones
Structural Classification
other families
Classification of Application Fields
Other Diseases
Plants
Naphthalene Quinones
Pteris livida Mett.
Disease Research Fields
|
FGFR
Necroptosis
Apoptosis
CDK
JNK
|
|
β,β-Dimethylacrylalkannin (Arnebin 1) is an orally active FGFR1 inhibitor (IC50=2.5 μM) and the main active component of Lithospermum erythrorhizon. β,β-Dimethylacrylalkannin blocks downstream signaling by binding to the ATP pocket of FGFR1, and regulates the CDK1/Cdc25C pathway and ROS-JNK axis, thereby inducing G2/M phase arrest, necrosis and apoptosis in cancer cells, and inhibiting tumor proliferation. β,β-Dimethylacrylalkannin also acts as a colistin adjuvant to disrupt the cell membrane of Gram-negative bacteria. β,β-Dimethylacrylalkannin exhibits significant tumor-inhibitory effects with no obvious toxicity in PDX models, but chronic exposure to high doses may alter the relative lung/liver weights of rats, while acute exposure to high doses causes responses such as reduced motor activity. β,β-Dimethylacrylalkannin finds wide application in studies related to hepatocellular carcinoma, colorectal cancer, colistin-resistant bacterial infections, hepatitis and psoriasis .
|
-
-
- HY-N0430
-
|
Coptisin
|
Alkaloids
Structural Classification
Classification of Application Fields
Coptis chinensis Franch.
Ranunculaceae
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-N0430A
-
|
|
Alkaloids
Structural Classification
Chelidonium majus
Classification of Application Fields
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Papaveraceae
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-N1428R
-
-
-
- HY-N1039A
-
-
-
- HY-N12124
-
-
-
- HY-N3000
-
|
|
Alkaloids
Structural Classification
Classification of Application Fields
Quinoline Alkaloids
Macleaya cordata (Willd.) R. Br.
Plants
Disease Research Fields
Papaveraceae
Source Classification
Cancer
|
JNK
IRE1
Akt
mTOR
YAP
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Fungal
|
|
6-Methoxydihydrosanguinarine is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .
|
-
-
- HY-122496
-
-
-
- HY-N12461
-
-
-
- HY-N3001
-
-
-
- HY-N0440R
-
|
|
Structural Classification
Terpenoids
Sesquiterpenes
Plants
Curcuma longa
Source Classification
Zingiberaceae
|
Reference Standards
Influenza Virus
NF-κB
5 alpha Reductase
Keap1-Nrf2
Lactate Dehydrogenase
Apoptosis
|
|
Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity .
|
-
-
- HY-N9942
-
-
-
- HY-N4164
-
-
-
- HY-B1357R
-
-
-
- HY-125132
-
-
-
- HY-N9968
-
-
-
- HY-126566
-
|
|
Natural Products
Microorganisms
Source Classification
|
Fungal
HDAC
Apoptosis
|
|
Trichostatin C is an inhibitor for histone deacetylase (HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
|
-
-
- HY-N9778
-
-
-
- HY-155852
-
-
-
- HY-N10670
-
-
-
- HY-N14881
-
-
-
- HY-N14866
-
-
-
- HY-N10798
-
-
-
- HY-N10394
-
-
-
- HY-122496R
-
-
-
- HY-N0421R
-
|
Cinobufagine (Standard)
|
Structural Classification
Animals
Steroids
Source Classification
|
Reference Standards
Apoptosis
|
|
Cinobufagin (Standard) is the analytical standard of Cinobufagin. This product is intended for research and analytical applications. Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
|
-
-
- HY-13451R
-
|
|
Microorganisms
Source Classification
|
Reference Standards
Bacterial
Antibiotic
|
|
Citric acid (Standard) is the analytical standard of Citric acid. This product is intended for research and analytical applications. Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice .
|
-
-
- HY-N3446
-
-
-
- HY-N2374R
-
-
-
- HY-N10018
-
-
-
- HY-N0047R
-
-
-
- HY-W009156R
-
|
Potassium citrate monohydrate (Standard)
|
Structural Classification
Ketones, Aldehydes, Acids
Guttiferae
Plants
Garcinia cambogia
|
Reference Standards
Apoptosis
Endogenous Metabolite
Bacterial
|
|
Citric acid tripotassium hydrate (Standard) (Potassium citrate monohydrate (Standard)) is the analytical standard of Citric acid tripotassium hydrate (HY-W009156). This product is intended for research and analytical applications. Citric acid tripotassium hydrate is a natural preservative and food tartness enhancer. Citric acid tripotassium hydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid tripotassium hydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid tripotassium hydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
-
- HY-B1295R
-
|
Litarex tetrahydrate (Standard)
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
Apoptosis
Endogenous Metabolite
Bacterial
Reference Standards
|
|
Lithium citrate (tetrahydrate) (Standard) is the analytical standard of Lithium citrate (tetrahydrate). This product is intended for research and analytical applications. Lithium citrate (Litarex) tetrahydrate is a natural preservative and food tartness enhancer. Lithium citrate tetrahydrate induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Lithium citrate tetrahydrate cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Lithium citrate tetrahydrate is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
|
-
-
- HY-W749442
-
|
|
Natural Products
Sphaeranthus indicus L.
Asteraceae
Plants
Source Classification
|
Microtubule/Tubulin
|
|
7a-Hydroxyfrullanolide has anticancer properties. 7a-Hydroxyfrullanolide reduces polymerization of α-, β-tubulin. 7a-Hydroxyfrullanolide preferrs to bind to β-tubulin over α-tubulin. 7a-Hydroxyfrullanolide also triggers DNA damage response arrests cells in the G2/M-phase. 7a-Hydroxyfrullanolide is an eudesmanolide sesquiterpene lactone (SL) and can be isolated from the flowering plants of the Asteraceae family .
|
-
-
- HY-N13294
-
|
TMJ-105
|
Terpenoids
Carpesium cernuum L.
Sesquiterpenes
Plants
Compositae
Source Classification
|
Apoptosis
JAK
STAT
p38 MAPK
JNK
ERK
|
|
Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC50 value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy .
|
-
-
- HY-N14734
-
|
|
Natural Products
Microorganisms
Source Classification
|
Apoptosis
Fungal
Microtubule/Tubulin
Mitosis
|
|
Disorazol A1 is an tubulin inhibitor with antifungal activity. Disorazol A1 functions by inhibiting tubulin polymerization, interfering with microtubule formation, blocking mitosis, thus arresting the cell cycle at the G2/M phase and inducing apoptosis. Disorazol A1 also exhibits an inhibitory effect against L929 mouse fibroblasts with an IC50 value of 3 pM. Disorazol A1 causes the accumulation of p53 protein in the cell nucleus. Disorazol A1 is promising for research of cancers .
|
-
- HY-N4189
-
-
- HY-160121
-
-
- HY-N1988R
-
-
- HY-W041470R
-
|
|
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
|
|
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
|
-
- HY-N15052
-
-
- HY-119736
-
-
- HY-N12331
-
-
- HY-118713
-
-
- HY-167237
-
-
- HY-N15306
-
|
|
Microorganisms
Ketones, Aldehydes, Acids
Phenols
Source Classification
|
Apoptosis
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-N17440
-
|
|
Quinones
Structural Classification
Juglandaceae
Phenols
Plants
Naphthalene Quinones
Juglans mandshurica
Source Classification
|
Apoptosis
Caspase
Bcl-2 Family
DNA/RNA Synthesis
Bacterial
Fungal
|
|
2-Methoxyjuglone, a naphthoquinone, is an apoptosis inducer. 2-Methoxyjuglone activates caspase-9 and caspase-3 via the mitochondrial cytochrome c-dependent intrinsic apoptosis cascade. 2-Methoxyjuglone increases pro-apoptotic Bax levels, decreases anti-apoptotic Bcl-2 levels, and promotes mitochondrial cytochrome c release. 2-Methoxyjuglone induces apoptosis morphological features, early apoptosis, S-phase and G2/M-phase cell cycle arrest, and DNA double-strand breaks. 2-Methoxyjuglone exerts activity against Gram-positive bacteria, pathogenic fungi, and phytopathogenic fungi. 2-Methoxyjuglone can be used for the research of hepatocellular carcinoma, osteosarcoma, colon adenocarcinoma, breast cancer, fungal infection, bacterial infection .
|
-
- HY-N16771
-
|
|
Structural Classification
Rutaceae
Coumarins
Phenylpropanoids
Plants
Clausena excavata N. L. Burman
Source Classification
|
Caspase
Apoptosis
Bcl-2 Family
Bacterial
VEGFR
|
|
Clausenidin is a selective inhibitor targeting apoptosis-related pathways, including the mitochondrial pathway and death receptor pathway, and vascular endothelial growth factor (VEGF). Clausenidin induces mitochondrial membrane depolarization by activating caspase-3, caspase-8 and caspase-9, upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-2. Clausenidin also inhibits VEGF expression and blocks angiogenesis, exerting anti-tumor activity. Clausenidin has inhibitory effects against Mycobacterium tuberculosis (MIC=200 μg/mL). Clausenidin can induce apoptosis in liver cancer cells, arrest the cell cycle in the G2/M phase, and inhibit tumor angiogenesis. Clausenidin can be used in the research of malignant tumors such as liver cancer .
|
-
- HY-N11846
-
|
|
Structural Classification
Natural Products
Glycyrrhiza glabra Linn.
Leguminosae
Plants
Source Classification
|
Apoptosis
Caspase
|
|
4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases .
|
-
- HY-N10342
-
|
|
Structural Classification
Flavonoids
Leguminosae
Phenols
Polyphenols
Plants
Isoflavones
Cajanus cajan (L.) Millsp.
Source Classification
|
Apoptosis
Bcl-2 Family
Caspase
PARP
Reactive Oxygen Species (ROS)
Bacterial
PI3K
Akt
NF-κB
P-glycoprotein
|
|
Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp. . Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections .
|
-
- HY-N3000A
-
|
|
Structural Classification
Alkaloids
Meconopsis simplicifolia (D. Don) Walp.
Quinoline Alkaloids
Plants
Papaveraceae
Source Classification
|
JNK
IRE1
Akt
mTOR
YAP
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Fungal
Caspase
DNA/RNA Synthesis
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6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-N1428S1
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Citric acid- 13C6 is the 13C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-N1428S
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Citric acid-d4 is the deuterium labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-N1428S3
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Citric acid- 13C3 is the 13C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-N1428S2
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Citric acid- 13C2 is the 13C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-N1428S6
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Citric acid-d4-1 is deuterated labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-W127841
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Citric acid-2,4- 13C2 is the 13C-labeled Citric acid (HY-N1428). Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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- HY-15149S2
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Romidepsin-d7 (FK 228-d7) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
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- HY-W747797
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Cinobufagine-d3 is the deuterium labeled Cinobufagin (HY-N0421). Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
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- HY-121605S
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RL71-d6 is a deuterium labeled RL71 (HY-121605). RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
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- HY-W724319
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Citric acid-d4 trisodium (Sodium citrate-d4) is the deuterium labeled Citric acid trisodium (HY-B2201). Citric acid trisodium (Sodium citrate) is a natural preservative and food tartness enhancer. Citric acid trisodium induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid trisodium cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid trisodium is also an acidulant, emulsifier, sequestrant and buffering agent widely used across many industries .
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| Cat. No. |
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Classification |
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- HY-147858
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PROTAC Synthesis
Alkynes
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-163099
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Alkynes
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P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
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- HY-134061
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Alkynes
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Arecaidine propargyl ester hydrobromide is an agonist of M2 muscarinic acetylcholine receptors and has the activity of inhibiting tumor cell proliferation. The application of arecaidine propargyl ester hydrobromide has shown that it can reduce the number of ovarian cancer cells in vitro and induce apoptosis and the production of reactive oxygen species (ROS) at specific concentrations. Arecaidine propargyl ester hydrobromide can also arrest cells at the G2/M phase of the cell cycle and increase the percentage of abnormal mitosis. Arecaidine propargyl ester hydrobromide is more sensitizing to ovarian surface epithelial cells with higher M2 receptor levels than to cancer cells. Arecaidine propargyl ester hydrobromide exhibits the effect of lowering arterial blood pressure when interacting with the cardiovascular system in a natural physiological state, indicating its potential pharmacological application .
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- HY-155541
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Alkynes
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Antitumor agent-110 (compound 13) is an anticancer imidazotetrazine with good permeability properties. Antitumor agent-110 arrests cell cycel at G2/M phase, and induces apoptosis . Antitumor agent-110 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-183628
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2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine
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BCN
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MEAP (2-(4-Morpholinoanilino-6-[(2-exo-norbornyl) amino)-purine) is a NEDD9-STAT3 modulator. MEAP disrupts NEDD9-STAT3 interaction, driving STAT3 Y705 dephosphorylation. MEAP induces G2/M phase arrest. MEAP can be used for the research of anaplastic thyroid cancer .
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15149G
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FK 228; FR 901228; NSC 630176
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HDAC
Apoptosis
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Cancer
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Romidepsin (GMP) (FK 228 (GMP)) is Romidepsin (HY-15149) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively . Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis .
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