目录号 | 产品详情 | 靶点 | |
---|---|---|---|
T78054 | Apoptosis | ||
JNJ-1013是一种选择性IRAK1降解剂,其对IRAK1、IRAK4、VHLFP的IC50值分别为72、443、1071nM。该化合物能诱导细胞凋亡(Apoptosis)并增加cleavagedPARP表达,同时降低IRAK1、p-IKBα、pSTAT3(Tyr705)的水平。 | |||
T79667 | PARP | ||
YCH1899为一种口服活性PARP抑制剂,其对PARP1/2的IC50均低于0.001 nM。该化合物对Olaparib和Talazoparib耐药的Capan-1细胞株(Capan-1/OP及Capan-1/TP细胞)表现出显著抗增殖能力,IC50分别为0.89 nM和1.13 nM。在大鼠体内,YCH1899展现优良的药代动力学属性。 | |||
T64223 | |||
RMS5 是一种汉防己碱类似物,是一种有效的 P-糖蛋白 (P-gp) 抑制剂。RMS5 对癌细胞具有显着的抗增殖和细胞毒作用。RMS5 略微降低抗凋亡 Bcl-2 家族蛋白 Bcl-XL 和 Mcl-1 的表达。RMS3 导致 PARP 裂解,这是细胞凋亡的标志物。RMS5 具有强抗癌特性。 | |||
T73403 | |||
Aviculin 是一种木聚糖苷,是一种有效的抗癌剂 (anticanceragent)。Aviculin 可降低 MCF-7 细胞代谢活性到 50% 以下,IC50为 75.47 μM。Aviculin 通过内在凋亡途径诱导乳腺癌细胞凋亡 (apoptosis)。Aviculin 增加了 caspase-9、caspase-7和 PARP 的表达。Aviculin 使 Bax/Bcl-2 的比值升高。 | |||
T79713 | HDAC | ||
JMJD3/HDAC-IN-1 (compound A5b) 是靶向 JMJD3 和 HDAC1(IC50=16 nM)的双重抑制剂。它能够促进 H3K27 高甲基化和 H3K9 高乙酰化,并通过裂解 caspase-7 和 PARP 导致细胞凋亡。此外,JMJD3/HDAC-IN-1 对抑制癌细胞克隆形成、迁移和侵袭也表现出有效性。 | |||
T71908 | |||
NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP +/- NU1085 (10 microM) for 72 h. | |||
T36703 | |||
CAY10760 is an inhibitor of the protein-protein interaction between RAD51 recombinase and BRCA2 (EC50= 19 μM in a cell-free competitive ELISA).1It decreases homologous recombination by 54% in wild-typeBRCA2-expressing BxPC-3 pancreatic cancer cells when used at a concentration of 20 μM. CAY10760 (20 μM) decreases proliferation of BxPC-3, as well as mutantBRCA2-expressing Capan-1, cancer cells when used alone or in combination with the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib . 1.Bagnolini, G., Milano, D., Manerba, M., et al.Synthetic lethality in pancreatic cancer: Discovery of a new RAD51-BRCA2 small molecule disruptor that inhibits homologous recombination and synergizes with olaparibJ. Med. Chem.63(5)2588-2619(2020) | |||
T70138 | |||
AZ0108 is an orally bioavailable, potent PARP1,2,6 inhibitor that potently inhibits centrosome clustering and is suitable for in vivo efficacy and tolerability studies. AZ0108 has been utilized as in vitro tools and in vivo probes to investigate the biological consequences of inhibiting centrosome clustering through PARP enzymes. AZ0108 is more selective in its enzyme inhibition profile and effects on cellular pathways and phenotypes. Specifically, AZ0108 inhibits PARPs 1, 2, and 6 with approximately 100-fold selectivity against PARP3 and TNKS1. Consistent with this lack of potencytowards tankyrase, AZ0108 is not active in a DLD-1 Wnt luciferase reporter assay. | |||
T28092 | |||
MPT0B206 is a novel tubulin polymerization inhibitor. MPT0B206 induced G2/M cell cycle arrest and the appearance of the mitotic marker MPM-2 in K562 and K562R cells, which is associated with the upregulation of cyclin B1 and the dephosphorylation of Cdc2. | |||
T10896 | Others | ||
CSRM617 is a selective small molecule inhibitor of the transcription factor ONECUT2 (OC2, the main regulator of androgen receptor). The Kd in SPR analysis is 7.43 uM, which can directly bind to the OC2-HOX domain. CSRM617 induces apoptosis by cleaving the |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
---|---|---|---|---|---|
TMPY-01188 | PARP Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
PARP Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 114.5 kDa and the accession number is A0A024R3T8.
|
|||||
TMPY-02465 | PARP Protein, Mouse, Recombinant (His) | Mouse | Baculovirus Insect Cells | ||
PARP Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with His tag. The predicted molecular weight is 115 kDa and the accession number is Q921K2.
|
|||||
TMPH-01943 | PARP4 Protein, Human, Recombinant (His) | Human | E. coli | ||
PARP4 Protein, Human, Recombinant (His) is expressed in E. coli.
|
|||||
TMPH-01880 | PARP2 Protein, Human, Recombinant (His) | Human | E. coli | ||
PARP2 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 72.2 kDa and the accession number is Q9UGN5.
|
|||||
TMPH-01882 | PARP9 Protein, Human, Recombinant (His) | Human | E. coli | ||
PARP9 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 30.0 kDa and the accession number is Q8IXQ6.
|
|||||
TMPH-01879 | PARP11 Protein, Human, Recombinant (His) | Human | E. coli | ||
Mono-ADP-ribosyltransferase that mediates mono-ADP-ribosylation of target proteins. Plays a role in nuclear envelope stability and nuclear remodeling during spermiogenesis. PARP11 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 41.0 kDa and the accession number is Q9NR21.
|
|||||
TMPY-02421 | PARP3 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Poly(ADP-ribose) polymerase 3 (PARP3) is an important member of the PARP family and shares high structural similarities with both PARP1 and PARP2. Poly(ADP-ribose) polymerase 3 (PARP3), a critical player in cellular response to DNA double-strand breaks (DSBs), plays an essential role in the maintenance of genome integrity. The ADP ribosyl transferase [poly(ADP-ribose) polymerase] ARTD3(PARP3) is a newly characterized member of the ARTD(PARP) family that catalyzes the reaction of ADP ribosylation, a key posttranslational modification of proteins involved in different signaling pathways from DNA damage to energy metabolism and organismal memory.
|
|||||
TMPH-01941 | PARP12 Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
PARP12 Protein, Human, Recombinant (His & Myc) is expressed in E. coli.
|
|||||
TMPH-01944 | PARP9 Protein, Human, Recombinant (His & Myc) | Human | HEK293 Cells | ||
PARP9 Protein, Human, Recombinant (His & Myc) is expressed in HEK293.
|
|||||
TMPH-01881 | PARP2 Protein, Human, Recombinant (GST & His) | Human | Baculovirus Insect Cells | ||
PARP2 Protein, Human, Recombinant (GST & His) is expressed in Baculovirus insect cells with N-GST and C-6xHis tag. The predicted molecular weight is 92.8 kDa and the accession number is Q9UGN5.
|
|||||
TMPH-01942 | PARP14 Protein, Human, Recombinant (His & Myc) | Human | HEK293 Cells | ||
PARP14 Protein, Human, Recombinant (His & Myc) is expressed in HEK293.
|
|||||
TMPY-02831 | Caspase-7 Protein, Human, Recombinant (His) | Human | E. coli | ||
Caspase 7, also known as caspase-7 and MCH3, belongs to the cysteine-aspartic acid protease (caspase) family. Caspases play a role in the signal transduction pathways of apoptosis, necrosis and inflammation. There are two major classes of caspases: initiators and effectors. The initiator isoforms (caspases-1,-4,-5,-8,-9,-10,-11,-12) are activated by, and interact with, upstream adaptor molecules through protein-protein interaction domains known as CARD and DED. Effector caspases (-3,-6,-7) are responsible for cleaving downstream substrates and are sometimes referred to as the executioner caspases. Caspase 7 exists in lung, skeletal muscle, liver, kidney, spleen, heart, and moderately in testis. Caspase 7 cannot be detected in the brain. Caspase 7 functions in the activation cascade of caspases responsible for apoptosis execution. It cleaves and activates sterol regulatory element binding proteins (SREBPs). It proteolytically cleaves poly(ADP-ribose) polymerase (PARP) at a '216-Asp- -Gly-217' bond. Overexpression promotes programmed cell death.
|