Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9698 |
UC2288
|
Mdm2; p53 | Apoptosis |
UC2288 是新型的、细胞通透性、口服有效的p21衰减试剂,基于索拉非尼的结构合成。在不依赖 于p53的情况下,它可以下调 p21 mRNA 的表达,降低 p21 蛋白水平,对 p21 蛋白的稳定性影响很小。它对VEGFR2 和 Raf 激酶没有抑制作用,即使在 10 μM。 | |||
T4459 |
PK11000
|
DNA Alkylator/Crosslinker | DNA Damage/DNA Repair |
PK11000 是一种烷化剂,可通过共价半胱氨酸修饰来稳定野生型和突变型p53的 DNA 结合结构域。 | |||
T9320 |
YK-3-237
B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid |
Sirtuin | Chromatin/Epigenetic; DNA Damage/DNA Repair |
YK-3-237 (B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid) 是 SIRT1 激活剂,靶向突变体 p53。它抑制三阴性乳腺癌细胞的增殖。 | |||
T3184 |
Kevetrin hydrochloride
Thioureidobutyronitrile HCl,thioureido butyronitrile hydrochloride,4-Isothioureidobutyronitrile hydrochloride |
Mdm2; p53 | Apoptosis |
Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) 是一种小分子,是肿瘤抑制蛋白 p53 的激活剂,具有潜在的抗肿瘤活性。 | |||
T64079 | Mutant p53 modulator-1 | ||
Mutant p53 modulator-1 是一种突变型 p53 调节剂。Mutant p53 modulator-1 能够阻碍含有 p53 突变的癌症的进展。 | |||
T6954 |
PRIMA-1
2,2-Bis(hydroxymethyl)-3-quinuclidinone,NSC-281668,PRIMA 1 |
Apoptosis; Others; Ferroptosis; Autophagy | Apoptosis; Autophagy; Others |
PRIMA-1 (NSC-281668) 是一种突变型 p53复活剂,可恢复 TP53 突变型甲状腺癌细胞对组蛋白甲基化抑制剂 3-Deazaneplanocin A 的敏感性。 | |||
T21648 |
CP-31398 dihydrochloride
CP 31398 dihydrochloride |
p53 | Apoptosis |
CP-31398 dihydrochloride 是一种 p53 稳定剂,可稳定 p53 的活性构象并促进具有突变型或野生型 p53 的癌细胞系中的 p53 活性。 | |||
T6910 |
NSC59984
|
p53 | Apoptosis |
NSC59984 是 p53 通路激活剂,可诱导突变 p53 蛋白降解和 p73 活化。它通过 MDM2 和泛素-蛋白酶体途径而诱导突变型 p53 蛋白降解。 | |||
T37042 |
SCH529074
SCH 529074 |
p53 | Apoptosis |
SCH529074 是 p53 的选择性激活剂 (Ki = 1 μM),可用于非小细胞肺癌的研究。 SCH529074 恢复突变 p53 功能并中断 HDM2 介导的野生型 p53 泛素化。 | |||
T4325 |
COTI-2
COTI 2,COTI2 |
Apoptosis; p53 | Apoptosis |
COTI-2是一种具有口服活性的低毒性抗癌药物,是 p53 突变体激活剂。它通过激活突变型 p53 和抑制PI3K/AKT/mTOR 途径发挥作用,通过 p53 依赖和非依赖机制在 HNSCC 中具有抗肿瘤活性。它诱导多种人肿瘤细胞凋亡,可将突变型 p53 转化为野生型构象。 | |||
T6611 |
NSC697923
2-[(4-methylphenyl)sulfonyl]-5-nitrofuran |
E1/E2/E3 Enzyme | Ubiquitination |
NSC-697923 (2-[(4-methylphenyl)sulfonyl]-5-nitrofuran), a potent inhibitor of UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13), exhibits its role in inducing cell death in neuroblastoma (NB) cells through two distinct mechanisms. In p53 wild-type NB cells, NSC-697923 promotes the nuclear importation of p53, thereby triggering cell death. Meanwhile, in p53 mutant NB cells, NSC-697923 activates the JNK-mediated apoptotic pathway, leading to cell death. Additionally, NSC-697923 inhibits DNA damage ... | |||
T4414 |
Eprenetapopt
APR-246,PRIMA-1Met |
Apoptosis; Others; Ferroptosis; p53; Autophagy | Apoptosis; Autophagy; Others |
Eprenetapopt (PRIMA-1Met) 是一种在 TP53突变细胞中恢复野生型 p53功能的小分子,可引发肿瘤细胞凋亡,还抑制硒蛋白硫氧还蛋白还原酶 1。 | |||
T60202 |
MMRi62
7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol |
Ferroptosis | Apoptosis |
MMRi62 (7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol) 是一种铁死亡 (ferroptosis) 诱导剂,靶向 MDM2-MDM4 (抑癌基因 p53 负调控因子)。MMRi62 对胰腺导管腺癌 (PDAC) 细胞显示出 p53 独立的促凋亡 (apoptosis) 活性,并诱导其自噬 (autophagy)。MMRi62 诱导铁死亡,伴随着活性氧增加和铁蛋白重链 (FTH1) 溶酶体降解。MMRi62 还可导致突变型 p53 的蛋白酶体降解,并对具有 KRAS 和 TP53 高频突变特征的原位异种移植 PDAC 小鼠模型具有体内药效。 | |||
T77768 |
BAY 1892005
|
p53 | Apoptosis |
BAY 1892005 是一种靶向 p53 凝聚体的 p53 蛋白调节剂,可用于研究与 p53 蛋白折叠错误相关的疾病 | |||
T74324 | NSC90616 | ||
NSC90616是一种p53突变拯救化合物。 | |||
T75517 | Colletofragarone A2 | ||
Colletofragarone A2,一种从真菌Colletotrichum sp. (13S020) 中分离得到的化合物,抑制p53突变蛋白和HSP90,因而具备抗癌活性。它促进p53突变蛋白的降解与聚合作用,并有能力抑制肿瘤在体内的生长。 | |||
T73533 | ADH-6 | ||
ADH-6,一种三吡啶酰胺化合物,消除突变p53 DBD聚集成核亚结构域的自组装,并靶向解离人类癌细胞中的突变p53聚集体。通过此过程,ADH-6恢复p53的转录活性,导致细胞周期停滞与细胞凋亡(apoptosis),展示了其研究癌症疾病的潜力。 | |||
T72770 | p53 Activator 5 | ||
p53 Activator 5 是一种有效的 p53激活剂,SC150 值 <0.05 mM。p53 Activator 5 可以结合突变体 p53 并恢复 p53 突变体结合 DNA 的能力。p53 Activator 5 具有抗肿瘤活性。 | |||
T72769 |
p53 Activator 3
|
||
p53 Activator 3,一种有效的p53激活剂,其SC150值<0.05 mM。该化合物能结合p53突变体并恢复其与DNA结合的功能,显示出抗肿瘤活性。 | |||
T74443 | ADH-6 TFA | ||
ADH-6 TFA为三吡啶酰胺类化合物,通过靶向并解离人类癌细胞中突变p53聚集体,阻止突变p53 DBD聚集成核亚结构域的自组装,从而恢复p53的转录活性。这一过程导致细胞周期停滞和细胞凋亡(apoptosis),显示出其在研究癌症疾病中的应用潜力。 | |||
T36934 |
PK7242 (maleate)
PK7242 (maleate) |
||
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 ... | |||
T73234 | USP7-IN-7 | ||
USP7-IN-7 是一种 USP7抑制剂,IC50值 <10 nM。USP7-IN-7 对 p53 突变癌细胞株、p53 野生型血液肿瘤和神经母细胞瘤细胞株具有低纳摩尔值的细胞毒性。USP7-IN-7 可用于肿瘤研究。 | |||
T78378 |
PK7088
|
Others | Others |
PK7088是一种结合了吡唑结构与特定肽序列的化合物,能够促使突变型p53恢复为具有野生型特性的形式,从而实现突变型p53的重激活。在癌症研究中,PK7088显示出其抗肿瘤活性。 | |||
T79013 | SLMP53-2 | ||
SLMP53-2是一种可以重建p53转录活性的突变p53再激活因子。该化合物通过促进mutp53-Y220C与Hsp70之间的作用,恢复了mutp53-Y220C的野生型构象和其DNA结合能力。此外,SLMP53-2能够诱导细胞周期停滞、细胞凋亡以及ER应激,展现出了其抗肿瘤的潜力。 | |||
T70941 |
CLR01 sodium
|
||
CLR01 is a molecular tweezer. CLR01 reduces aggregated, pathologic, and seeding-competent α-synuclein in experimental multiple system atrophy. CLR01 inhibits aberrant superoxide dismutase 1 (SOD1) self-assembly in vitro and in the G93A-SOD1 mouse model of ALS. CLR01 inhibits Ebola and Zika virus infection. CLR01 Stabilizes a Disordered Protein-Protein Interface. CLR01, Modulates Aggregation of the Mutant p53 DNA Binding Domain and Inhibits Its Toxicity. | |||
T83082 | Anticancer agent 168 | ||
Anticanceragent 168(compound d16)是一种DNA2抑制剂。该化合物能够促进细胞凋亡(apoptosis),引起细胞周期在S期显著停滞,并在含mutp53肿瘤中显示出抗癌效应,有助于克服化疗耐药性。 | |||
T35696 |
Olomoucine II
|
||
Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively... | |||
T78715 |
MS78
|
||
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。 | |||
T35874 |
CC260
|
||
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph... |