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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1767 |
BMH-21
BMH21 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
BMH-21 是一种小分子 DNA 嵌入剂,可结合核糖体 DNA 并抑制 RNA 聚合酶 I (Pol I) 转录,具有抗癌活性。 | |||
T7318 |
Elimusertib
BAY-1895344 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Elimusertib (BAY-1895344) 是一种可口服的选择性ATR 抑制剂,IC50值为 7 nM。它具有抗肿瘤活性,可研究实体瘤和淋巴瘤。 | |||
T14141 |
AGI-24512
|
Others; Methionine Adenosyltransferase (MAT) | Chromatin/Epigenetic; Others |
AGI-24512 是一种甲硫氨酸腺苷转移酶 2A 抑制剂,在体外能够阻断 MTAP 缺失的癌细胞的生长,可用于研究癌症。 | |||
T23974 |
DDRI-18
DDRI18,DDRI 18 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
DDRI-18 是一种调节 DNA 损伤反应的新型小分子抑制剂,具有增敏活性和抗癌活性,抑制非同源末端连接 (NHEJ) DNA 修复过程,增强抗癌 DNA 损伤化合物的细胞毒性作用。 | |||
T23284 |
Ryuvidine
|
Histone Demethylase; Histone Methyltransferase; CDK | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Ryuvidine 是一种 KDM5A 和 SETD8 双重抑制剂,是一种 DNA 损伤反应的诱导剂,具有潜在的抗癌活性,抑制 H4K20 甲基化,抑制 CDK4,可用于研究乳腺癌和红斑病。 | |||
T9849 |
HQ461
|
CDK; Molecular Glues | Cell Cycle/Checkpoint; PROTAC |
HQ461 是一种分子胶,可促进 CDK12-DDB1 相互作用并触发 cyclin K 降解, cyclin K 的降解会损害 CDK12 的功能,导致 CDK12 底物磷酸化降低、DNA 损伤反应基因下调和细胞死亡。 | |||
T23095 |
NU 9056
NU9056 |
Histone Acetyltransferase | Chromatin/Epigenetic |
NU 9056 是一种有效且选择性的 KAT5 组蛋白乙酰转移酶抑制剂,IC50 为 2 µM。 NU 9056 阻断 DNA 损伤反应并抑制前列腺癌细胞系中的蛋白质乙酰化。 | |||
T37450 |
SSK1
|
p38 MAPK | MAPK |
SSK1 是一种选择性杀死衰老细胞的化合物,是一种针对 β-galactosidase 的前体,可减轻机体炎症反应。SSK1 可激活衰老细胞中 p38 MAPK 和 MKK3/MKK6 的磷酸化水平,促使衰老细胞线粒体 DNA 损伤。 | |||
T26872 |
BMVC4
BMVC 4,BMVC-4 |
||
BMVC4 is a G-quadruplex stabilizer. BMVC4 induces senescence by activation of pathways of response to DNA damage that was independent of its telomerase inhibitory activity. | |||
T10557 | BLM-IN-1 | Others | Others |
BLM-IN-1 is an effective Bloom syndrome protein (BLM) inhibitor (KD: 1.81 μM; IC50: 0.95 μM). It induces DNA damage response, apoptosis and proliferation arrest in cancer cells | |||
T39795 |
Tricarbonyldichlororuthenium(II) dimer
CORM-2 |
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Tricarbonyldichlororuthenium(II) dimer, a pharmacological CO donor, prevents ischemia/reperfusion (I/R)-induced oxidative damage to the gastric mucosa by enhancing gastric blood flow (GBF) and reducing DNA oxidation and systemic inflammatory response. | |||
T36701 | Phosphoramide mustard (cyclohexanamine) | ||
Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide , with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].Phosphoramide mustard cyclohexanamine destroys rapidly dividing ce... | |||
T36704 |
CCT241533 dihydrochloride
CCT 241533 dihydrochloride |
||
Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes. Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID:21186793 | |||
T78077 |
E235
|
Others | Others |
E235是一种调控转录因子4(ATF4)表达的激活剂。该化合物可以通过启动综合应激反应(ISR)和DNA损伤应答信号来降低细胞的活性。E235显示出抗增殖活性,适用于肿瘤学研究。 | |||
T73299 |
APE1-IN-2
|
Apoptosis | Apoptosis |
APE1-IN-2(compound AP1)是一种具有抗癌活性的Pt(IV)前体,靶向BER关键蛋白APE1。该化合物能诱导细胞内铂的积累,并激活DNA损伤反应及凋亡信号。 | |||
T78959 | ATR-IN-23 | ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
ATR-IN-23 (Compound 34) 是一种选择性ATR抑制剂,其IC50为 1.5 nM。该化合物对LoVo细胞表现出抗增殖活性,并对HT-29细胞产生合成致死效果,适用于研究DNA损伤反应(DDR)缺陷癌症。 | |||
T60478 |
BTX161
|
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BTX161 是沙利度胺类似物。BTX161是有效的 CKIα降解剂。在人类 AML 细胞中,BTX161 比来那度胺更好地介导 CKIα 降解,激活 DNA 损伤反应 (DDR) 和 p53,并能稳定 p53 拮抗剂 MDM2。 | |||
T81640 |
NSC15520
|
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NSC15520是一种小分子RPA抑制剂,特异性结合RPA的N端DNA结合域(DBD),阻断其与p53或RAD9的相互作用。它还能够抑制双链DNA(dsDNA)寡核苷酸的螺旋不稳定性,影响DNA复制、修复、重组及损伤反应信号。 | |||
T37729 |
IMP-1700
|
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IMP-1700 is an inhibitor of bacterial DNA repair.1It potentiates the activity of the quinolone antibiotic ciprofloxacin against methicillin-resistantS. aureus(MRSA) with a combination index value of 0.7. IMP-1700 inhibits the ciprofloxacin-induced bacterial SOS response, a process that repairs DNA damage, in a reporter assay in a concentration-dependent manner. It is also active againstE. coli, as well as methicillin-resistant and -sensitive S. aureus, when used alone (EC50s = 0.5, 0.21, and 3.8... | |||
T78715 |
MS78
|
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MS78为一种乙酰化靶向嵌合体(AceTAC),其功能是招募组蛋白乙酰转移酶p300/CBP以乙酰化p53肿瘤抑制蛋白的p53Y220C突变体。通过该作用,MS78能够上调TRAIL凋亡基因,同时下调DNA损伤反应信号通路。此化合物结构包含CBP/p300结合物、p53Y220C结合物及linker。 | |||
T73558 | W1131 | ||
W1131 是一种有效的STAT3抑制剂,可引发铁死亡。W1131 在胃癌皮下异种移植模型、类器官模型和 PDX 模型中抑制癌症进展。W1131 有效减轻癌细胞对 5-FU 化学耐药性。W1131 调节细胞周期、DNA 损伤反应和氧化磷酸化,包括IL6-JAK-STAT3通路和铁死亡 (ferroptosis) 通路。 | |||
T36934 |
PK7242 (maleate)
PK7242 (maleate) |
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The protein p53, often called the 'guardian of the genome,' is a transcription factor that is activated in response to cellular stress (low oxygen levels, heat shock, DNA damage, etc.) and acts to prevent further proliferation of the stressed cell by promoting cell cycle arrest or apoptosis. Its role as a tumor suppressor is evident by the observation that approximately 50% of human tumors have mutated or non-functional p53. PK7242 is an inducer of reactivation of mutant p53 in cancer cells. In ... | |||
T62651 | ATR-IN-11 | ||
ATR-IN-11 (Compound Hit01) 是一种共济失调毛细血管扩张症和 Rad3 相关 (ATR) 激酶的有效抑制剂。ATR 激酶是 DNA 损伤反应 (DDR) 中的一个关键调节蛋白,负责感知复制压力 (RS)。ATR-IN-11 是一种有希望的先导化合物,能够用于发现后续针对 ATR 激酶的药物。 ATR-IN-11具有潜力进行癌症疾病的研究。 | |||
T80847 | W1131 TFA | STAT | JAK/STAT signaling; Stem Cells |
W1131 TFA 是一种抑制STAT3并诱导铁死亡(ferroptosis)的有效化合物。在胃癌的皮下异种移植模型、类器官模型以及PDX模型中,它都能显著阻止疾病的发展。此外,W1131能有效缓解癌细胞对5-FU的化学耐药性。该化合物还通过调节IL6-JAK-STAT3和铁死亡(ferroptosis)通路来影响细胞周期、DNA损伤响应和氧化磷酸化过程。 | |||
T64022 | Antitumor agent-37 | ||
Antitumor agent-37 表现出有效的抗增殖和抗转移效果。Antitumor agent-37 能够诱导严重的 DNA 损伤,进而导致 γ-H2AX 和 p53 的高表达。Antitumor agent-37 可利用线粒体凋亡通路 Bcl-2/Bax/caspase3,诱导肿瘤细胞凋亡 (apoptosis)。Antitumor agent-37 可以抑制 PD-L1 的表达,提高肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞,明显改善免疫反应。 | |||
T74393 | Antitumor agent-36 | ||
Antitumor agent-36 具有有效的抗增殖和抗转移活性,能诱导严重的 DNA 损伤,并通过增加 γ-H2AX 和 p53 的表达促进肿瘤细胞通过 Bcl-2/Bax/caspase3 线粒体凋亡通路的 (apoptosis)。此外,Antitumor agent-36 还能通过抑制 PD-L1 的表达显著增加肿瘤组织中 CD3+ 和 CD8+ T 浸润细胞,从而改善免疫反应。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2915 |
Bardoxolone
RTA 401,齐墩果烷三萜化合物,CDDO |
Others; Nrf2 | Immunology/Inflammation; Others |
Bardoxolone (CDDO) 是新型核调节因子激活剂。 |