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Cat. No. | Product Name | Target | Signaling Pathways |
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T11282 |
FGTI-2734
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Transferase | Metabolism |
FGTI-2734 是 有效的RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT-1) 抑制剂,IC50s 分别为 250 nM 和 520 nM。 它可以阻断 KRAS 的膜定位,从而解决 KRAS 耐药性问题,并抑制突变的 KRAS 胰腺肿瘤。 | |||
T9167 |
PF-9363
CTX-3648 |
Histone Acetyltransferase | Chromatin/Epigenetic |
PF-9363 (CTX-3648) 是一种有效且高选择性的 KAT6A/KAT6B 抑制剂,可用于癌症研究。 | |||
T2069L |
TH287 hydrochloride
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DNA/RNA Synthesis; MTH1 | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
TH287 hydrochloride 是一种选择性MTH1抑制剂,IC50值为 0.8 nM。它可用于治疗癌症的研究。 | |||
T60372 |
ALDH3A1-IN-1
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ALDH3A1-IN-1 (Compound 18) 是一种有效的ALDH3A1抑制剂,IC50为 1.61 μM。ALDH3A1-IN-1 比 DEAB 更有效地对抗患者来源的原发性前列腺肿瘤上皮细胞,无论是作为单药或与多西紫杉醇联合治疗。 | |||
T35822 |
CAY10722
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CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM). SIRT3 is involved in modulating metabolic homeostasis as a NAD+-dependent protein deacetylase in the mitochondria. SIRT3 functions as either an oncogene or tumor suppressor, depending on cancer cell type. High SIRT3 expression in patient-derived esophageal cancer tissues is associated with shorter survival and, in mice, downregulation leads to a lower tumor load. In contrast, low SIRT3 expression in patie... | |||
T83716 |
KSL-128114 TFA
Ac-rRrGrKkRrSHWX1X2DI-OH (X1=tert-Leucine; X2=Cyclohexylglycine) |
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KSL-128114是一种对膜调节剂syntenin的肽抑制剂(Ki = 300 nM)。它能够依赖浓度降低A2058黑色素瘤和患者来源的多形性胶质母细胞瘤(GBM)细胞的存活率。在使用患者来源的GBM细胞并在颅内植入前用KSL-128114培养的患者衍生异种移植(PDX)小鼠模型中,KSL-128114(50 µM)提高了动物的存活时间。 | |||
T70134 |
L-778123 Dihydrochloride
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L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed. | |||
T11282L |
FGTI-2734 mesylate (1247018-19-4 free base)
FGTI-2734 mesylate |
Others | Others |
FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors. | |||
T35670 | Miro1 Reducer | ||
Promotes proteasomal degradation of Miro1 (mitochondrial Rho GTPase 1). Reduces Miro1 levels in fibroblasts from Parkinson's disease (PD) patients (IC50 = 7.8 μM). Exhibits no significant effect on related outer mitochondrial membrane protein Mitofusin. Reduces stress-induced degeneration of dopaminergic neurons derived from PD patient iPSCs. Rescues age-dependent neuronal loss and prolongs lifespan in fly PD models. | |||
T79461 | YK-029A | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
YK-029A为口服活性的EGFR突变抑制剂,特异性针对EGFRT790M及EGFRex20ins。该化合物在PDX模型上对肿瘤展现良好的抑制效果,显示出明显的抗肿瘤活性。 | |||
T36275 |
xStAx-VHLL
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Selective peptide-based β-catenin Degrader. Comprises a β-catenin-targeted stapled peptide, xStAx, linked to a VHL-binding peptide. Reduces β-catenin levels in HEK293T cells and colorectal cancer cell lines. Selectively degrades β-catenin over other Wnt signaling pathway components. Inhibits tumor growth in APCmin/+ mice, with constitutively active Wnt signaling, and reduces survival of patient-derived colorectal cancer cell organoids. | |||
T66481 |
TG-693
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TG693, an orally available inhibitor of CLK1, promotes the skipping of the endogenous mutated exon 31 in Duchenne muscular dystrophy (DMD) patient-derived cells and increased the production of the functional exon 31-skipped dystrophin protein. | |||
T62676 | DS89002333 | ||
DS89002333 是一种强效的、口服具有活力的 PRKACA 抑制剂 (IC50: 0.3 nM)。DS89002333 在表达 DNAJB1-PRKACA 融合基因的 FL-HCC 患者源性异种移植模型中具有良好的抗肿瘤作用。DS89002333 能够用于研究纤维化肝细胞癌 (FL-HCC)。 | |||
T73429 |
VT02956
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VT02956 是一种LATS 抑制剂 (IC50: LATS1 为 0.76 nM,LATS2 为 0.52 nM)。VT02956 靶向Hippo 信号通路。VT02956 抑制 ER+ 乳腺癌细胞系和患者来源的肿瘤类器官的生长和 ESR1 表达。 | |||
T35481 |
DD 03-171
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Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models. | |||
T76791 | Seribantumab | ||
Seribantumab (MM 121) 是一种完全人 IgG2单克隆抗体,靶向 HER3。Seribantumab 阻断 ErbB 家族成员及其下游信号的激活。Seribantumab 在体内、外抑制乳腺癌、肺癌和卵巢癌患者源性癌症模型中神经调节蛋白 (NRG1) 融合依赖的肿瘤发生。 | |||
T83912 |
HR68
PP21 |
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HR68是一种抗癌化合物,是过氧化物酶体增殖物激活受体(PPAR)激动剂非诺贝酯的衍生物。它能降低LN-229胶质母细胞瘤细胞的存活率(IC50 = 1.17 µM)。HR68能够穿越血脑屏障,在对替莫唑胺耐药的原位患者衍生的异种移植(PDX)小鼠胶质母细胞瘤模型中发挥作用。 | |||
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。 | |||
T78877 |
MTX-241F
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EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MTX-241F是一种选择性小分子抑制剂,针对EGFR和PI3激酶家族。其具备穿透血脑屏障的能力,能够持续控制肿瘤生长。在来源于患者的DIPG神经球中,MTX-241F展示了与放射疗法协同增效的特性,适用于研究弥漫性内源性桥脑胶质瘤(DIPG)。 | |||
T36451 |
1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) (sodium salt)
1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) (sodium salt),biotin-cap-DPPE |
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1,2-Dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) is a biotinylated phospholipid. It has been used in PEGylated polyamidoamine-dendrimer-conjugated supported lipid bilayers (SLB) to isolate circulating tumor cells and tumor cell microembolis from patient-derived blood by antibody-coated microfluidics. [1] It has also been used as a component of SLBs to detect protein-ligand binding with ortho-conjugated Texas Red DHPE. [2] In addition, 1,2-dipalmitoyl-sn-glycero-3-PE-N-(cap biotin) has been used i... | |||
T77012 | Flotetuzumab | ||
Flotetuzumab (MGD006; S80880) 是一种双特异性 CD123/CD3双亲和再靶向 (DART) 抗体。Flotetuzumab 通过同时结合靶细胞的 CD123和效应 T 细胞的CD3,而重新激活 T 细胞,导致 T 细胞介导的靶细胞的细胞毒性。Flotetuzumab 对小鼠中急性髓系白血病 (AML) 患者来源异种移植物 (PDX) 模型具有抑制效力。 | |||
T79405 |
PARP1-IN-15
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PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
PARP1-IN-15(Compound 6)是一款针对PARP1的抑制剂,能够抑制坦聚合酶(TNKS)并促进DNA双链断裂损伤。该化合物在诱导肿瘤细胞凋亡(apoptosis)方面具有显著作用,且在三阴性乳腺癌(TNBC)细胞及来源于TNBC患者的类器官中显示出抗癌活性,适用于探究BRCA1突变状态下的TNBC研究。 | |||
T83930 |
SJ 11646
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SJ11646是一种高效的LCK(淋巴细胞特异性蛋白酪氨酸激酶)降解剂(PROTAC;DC50= 0.00838 pM)。该化合物由Dasatinib作为LCK配体,以及基于苯基谷氨酰亚胺的cereblon结合体组成。它在体外对LCK激活的T细胞急性淋巴细胞白血病(T-ALL)细胞株和初级白血病样本展现出细胞毒性。在体内,SJ11646在源自患者的T-ALL异种移植模型中显示出抗白血病效果。 | |||
T36235 |
5-Chlorouracil
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5-Chlorouracil is a chlorinated derivative of the pyrimidine nucleoside base uracil . In vivo, it is converted into chlorodeoxyuridine, which is mutagenic and genotoxic.1 Uracil is chlorinated at the 5 position in a cell-free myeloperoxidase, peroxide, and chloride system in which hypochlorous acid is formed.2 5-Chlorouracil has been found in human neutrophils stimulated with phorbol 12-myristate 13-acetate in vitro and in inflammatory human exudate isolated from sites of superficial infection. ... | |||
T35940 |
Darinaparsin
Dimethylarsinic glutathione,Darinaparsin |
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Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 µM) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 µM), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 µM, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T83281 | 6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine | ||
6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine 显著影响细胞器特性,涉及早期内体、线粒体及自噬体(源自帕金森病患者的嗅觉细胞)。 |