Search Result
Results for "
H2AX
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-18174
-
Prexasertib
Maximum Cited Publications
33 Publications Verification
LY2606368
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
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Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity [2].
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-
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- HY-12037A
-
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ON-01910
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Polo-like Kinase (PLK)
PI3K
Apoptosis
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Cancer
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Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle [2]. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
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-
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- HY-W1126504
-
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MC339
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Notch
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Cancer
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ETN029 (MC339) is a selective DLL3 ligand. ETN029 labeled with 225Ac has dose-dependent cytotoxicity in SCLC, NEPC and metastatic melanoma cells and increases the phosphorylation of H2AX expression. ETN029 labeled with 177Lu shows rapid uptake persistent tumor retention and favorable tumor-to-kidney ratio. ETN029 can be used for cancers like SCLC and NEPC imaging and research [2].
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- HY-123834
-
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FLAP
ATM/ATR
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Cancer
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FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg 2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers .
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- HY-N0316
-
|
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JAK
NF-κB
Reactive Oxygen Species (ROS)
Apoptosis
VEGFR
c-Myc
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Cancer
|
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Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway [2] .
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- HY-18174A
-
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LY2606368 dihydrochloride
|
Checkpoint Kinase (Chk)
Apoptosis
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Cancer
|
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Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity [2].
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- HY-101089
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RHPS4
5 Publications Verification
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Telomerase
Apoptosis
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Cancer
|
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RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer [2].
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- HY-122181
-
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Histone Methyltransferase
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Cancer
|
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OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
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- HY-12037
-
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ON-01910 sodium
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Polo-like Kinase (PLK)
PI3K
Apoptosis
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Cancer
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Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle [2]. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
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- HY-117693
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ATM/ATR
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Cancer
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(E/Z)-Mirin is a mixture of (E)-Mirin and Mirin ((Z)-Mirin) (HY-19959) configurations. Among them, Mirin is an inhibitor of MRN (Mre11-Rad50-Nbs1). Mirin prevents MRN-dependent ATM activation without affecting ATM protein kinase activity [2].
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- HY-163944
-
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DNA/RNA Synthesis
Molecular Glues
CDK
Apoptosis
RAD51
ATM/ATR
PARP
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Cancer
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LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer [2].
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- HY-N2445
-
|
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Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
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Cancer
|
|
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer [2] .
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- HY-122182
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Histone Methyltransferase
Apoptosis
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Cancer
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OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
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- HY-103241
-
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Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Neurological Disease
Cancer
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Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response [2]. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
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- HY-18174E
-
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LY2606368 dimesylate
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
|
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Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity [2].
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- HY-122181B
-
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Histone Methyltransferase
|
Cancer
|
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OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
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- HY-158975
-
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Casein Kinase
VRK
|
Cancer
|
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VRK1/CK1-IN-1 (compound 36) is a dual VRK1 and CK1 family inhibitor, with a Ki of 37.9 nM against human VRK1, 8.3 nM against human CK1δ, and 7.8 nM against human CK1ε. VRK1/CK1-IN-1 exhibits extremely low activity against VRK2. VRK1/CK1-IN-1 can be used in studies related to p53-deficient tumors .
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- HY-113041
-
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PGA2; Medullin
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Apoptosis
Caspase
PARP
ERK
MDM-2/p53
JNK
HSV
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Infection
Cancer
|
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Prostaglandin A2 (PGA2) is a Cyclopentenone prostaglandin. Prostaglandin A2 induces Caspase-dependent Apoptosis, activates p53. Prostaglandin A2 activates ERK2 and JNK1/SAPK. Prostaglandin A2 shows antiviral activity against HSV-1. Prostaglandin A2 has anti-tumor effects. Prostaglandin A2 can be used for the research of colorectal cancer, colorectal carcinoma, breast carcinoma, and herpetic keratitis [2] .
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- HY-RS05957
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Small Interfering RNA (siRNA)
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Others
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H2AX Human Pre-designed siRNA Set A contains three designed siRNAs for H2AX gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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H2AX Human Pre-designed siRNA Set A
H2AX Human Pre-designed siRNA Set A
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- HY-132972
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TrxR
Reactive Oxygen Species (ROS)
Autophagy
Atg8/LC3
Beclin1
p62
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Cancer
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TrxR-IN-2 is a thioredoxin reductase (TrxR) inhibitor. TrxR-IN-2 increases reactive oxidative species (ROS) levels and decreases mitochondrial transmembrane potential levels. TrxR-IN-2 triggers DNA damage via H2AX regulation, and induces autophagy via LC3, beclin-1, and p62 regulation. TrxR-IN-2 can be used for the research of drug-resistant hepatocellular carcinoma[1].
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- HY-RS16644
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Small Interfering RNA (siRNA)
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Others
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H2ax Mouse Pre-designed siRNA Set A contains three designed siRNAs for H2ax gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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H2ax Mouse Pre-designed siRNA Set A
H2ax Mouse Pre-designed siRNA Set A
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- HY-122860
-
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TOPK
Apoptosis
c-Myc
MDM-2/p53
FAK
Src
Mitosis
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Cancer
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SKLB-C05 is a novel selective, orally active TOPK inhibitor, with an IC50 of 0.5 nM. SKLB-C05 selectively inhibit TOPK kinase. SKLB-C05 induces Apoptosis, downregulates c-Myc, γ-H2AX, activates p53, blocks FAK/Src medicated migration-related signaling. SKLB-C05 disturbs cell mitosis. SKLB-C05 shows anticancer activity only against TOPK-positive colorectal cancer .
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- HY-RS23078
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Small Interfering RNA (siRNA)
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Others
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H2ax Rat Pre-designed siRNA Set A contains three designed siRNAs for H2ax gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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H2ax Rat Pre-designed siRNA Set A
H2ax Rat Pre-designed siRNA Set A
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- HY-175700
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Topoisomerase
Apoptosis
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Cancer
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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) .
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- HY-W414334
-
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DNA/RNA Synthesis
Fluorescent Dye
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Cancer
|
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ICR-191 dihydrochloride enhances Cisplatin (HY-17394)- DNA binding and sensitizes cells to cisplatin. ICR-191 dihydrochloride induces a significant increase in the expression of phosphorylated H2AX (γH2AX), particularly in DNA-replicating cells. ICR-191 dihydrochloride can be used for the study of leukemia [2].
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- HY-121777
-
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DNA/RNA Synthesis
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Cancer
|
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SFOM-0046 arrests cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into γ-H2AX. SFOM-0046 induces DNA damages. SFOM-0046 is a potent anticancer agent .
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- HY-174989
-
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ATM/ATR
Apoptosis
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Cancer
|
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ATM-IN-2 is a selective and orally active ATM inhibitor with an IC50 of 4 nM. ATM-IN-2 exhibits excellent kinase selectivity (>700-fold over PIKK family members). ATM-IN-2 exerts its anti-tumor effect by inhibiting ATM phosphorylation and the downstream signaling pathways (p53, H2AX), and promotes cell apoptosis. ATM-IN-2 can be used for the study of chemosensitizer candidate such as colon cancer .
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- HY-N0316R
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JAK
Reference Standards
NF-κB
Reactive Oxygen Species (ROS)
Apoptosis
VEGFR
c-Myc
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Cancer
|
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Mollugin (Standard) is the analytical standard of Mollugin. This product is intended for research and analytical applications. Mollugin is an orally active and potent NF-κB inhibitor. Mollugin induces S-phase arrest of HepG2 cells, and increased intracellular reactive oxygen species (ROS) levels. Mollugin induces DNA damage in HepG2 cells, as well as an increase in the expression of p-H2AX. Mollugin shows anti-cancer effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 (bone morphogenetic protein 2) via the p38-Smad signaling pathway [2] .
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- HY-18174H
-
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LY2606368 lactate
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Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
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Cancer
|
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Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity [2].
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- HY-122181A
-
|
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Histone Methyltransferase
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Cancer
|
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OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
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- HY-162985
-
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CDK
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Cancer
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JHD205 is a CDK4/6 inhibitor that induces apoptosis and DNA damage. JHD205 inhibits DNA repair by upregulating Caspase3 and p-H2AX. JHD205 has superior potency to Abemaciclib (HY-16297A) in a xenograft chick embryo breast cancer model. .
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- HY-168877
-
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MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
|
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FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .
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- HY-117688
-
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HDAC
Topoisomerase
Apoptosis
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Cancer
|
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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 .
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- HY-145289
-
|
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Apoptosis
|
Cancer
|
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Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
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- HY-145288
-
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Apoptosis
|
Cancer
|
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Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .
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- HY-18174B
-
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LY2606368 Mesylate Hydrate; LY2940930
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Checkpoint Kinase (Chk)
Apoptosis
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Cancer
|
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Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity [2].
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- HY-18174C
-
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LY2606368 mesylate
|
Checkpoint Kinase (Chk)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
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Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity [2].
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- HY-181557
-
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DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Apoptosis
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Cancer
|
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SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC50=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC50=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors .
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- HY-181018
-
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Topoisomerase
PAK
Bcl-2 Family
IAP
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
|
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Topo I/DDX5-IN-1 (Compound A10) is a Topo I and DDX5 inhibitor. Topo I/DDX5-IN-1 inhibits Topo I activity, binds to DDX5, and suppresses DDX5 function. Topo I/DDX5-IN-1 increases expression of γ-H2AX and p21, suppresses the expression of antiapoptotic proteins (Bcl-2 and XIAP), stimulates ROS generation, and triggers Apoptosis. Topo I/DDX5-IN-1 exhibits anticancer activity against pancreatic cancer, non-small cell lung cancer, skin cancer, and colorectal cancer .
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- HY-183330
-
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Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
MDM-2/p53
Caspase
Bcl-2 Family
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Cancer
|
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Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC50 of 8.99 μM against Topo I and an IC50 of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of γ-H2AX, p53, activated caspase-9, Bax and activated caspase-3, while downregulating the expression of Bcl-2. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer .
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- HY-181678
-
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DNA-PK
HDAC
Apoptosis
Mitochondrial Metabolism
DNA/RNA Synthesis
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Cancer
|
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DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia .
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- HY-101089R
-
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Telomerase
Reference Standards
Apoptosis
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Cancer
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RHPS4 (Standard) is the analytical standard of RHPS4 (HY-101089). This product is intended for research and analytical applications. RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer [2].
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- HY-103241R
-
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Reference Standards
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
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Neurological Disease
Cancer
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|
Ro 90-7501 (Standard) is the analytical standard of Ro 90-7501 (HY-103241). This product is intended for research and analytical applications. Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response [2]. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner . Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells .
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- HY-167237
-
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Apoptosis
Caspase
CDK
PARP
Bcl-2 Family
ERK
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Cancer
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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 .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0316
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-
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- HY-N2445
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Structural Classification
Classification of Application Fields
Piperaceae
Plants
Chalcones
Flavonoids
other families
Phenols
Polyphenols
Piper methysticum G.Forst.
Disease Research Fields
Source Classification
Cancer
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Apoptosis
Akt
JNK
PERK
Caspase
PARP
MDM-2/p53
IAP
Reactive Oxygen Species (ROS)
SOD
FABP
Autophagy
AMPK
mTOR
GLUT
EGFR
PI3K
HSP
VEGFR
FAK
|
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Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer [2] .
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- HY-N0316R
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- HY-167237
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* This product has been "discontinued".
Optimized version of product available:
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- HY-RS05957
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siRNAs
Human Pre-designed siRNA Sets
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H2AX Human Pre-designed siRNA Set A contains three designed siRNAs for H2AX gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS16644
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siRNAs
Mouse Pre-designed siRNA Sets
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H2ax Mouse Pre-designed siRNA Set A contains three designed siRNAs for H2ax gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS23078
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siRNAs
Rat Pre-designed siRNA Sets
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H2ax Rat Pre-designed siRNA Set A contains three designed siRNAs for H2ax gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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