Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5469 |
K-Ras-IN-1
|
Raf; Ras | GPCR/G Protein; MAPK |
K-Ras-IN-1 是K-Ras 抑制剂。K-Ras-IN-1 能与 K-Ras (WT)、K-Ras (G12D)、K-Ras (G12V) 和 H-Ras 结合。它对胰腺癌、结肠癌和肺癌的具潜在的研究价值。 | |||
T8659 |
K-Ras-PDEδ-IN-1
|
PDE | Metabolism |
K-Ras-PDEδ-IN-1 是新型的 K-Ras-PDEδ 抑制剂,它能够以低纳摩尔Kd8 nM 与 PDEδ 的法尼基结合袋竞争性结合。 | |||
T11735 |
K-Ras G12C-IN-1
|
Phosphatase | Metabolism |
K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C. | |||
T38050 |
CP-609754
|
Transferase | Metabolism |
CP-609754 是高效的、可逆的法尼基转移酶抑制剂,对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。 | |||
T18056 |
K-Ras ligand-Linker Conjugate 3
|
Others | Others |
K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound that consists of a ligand for K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential in the synthesis of PROTAC K-Ras Degrader-1, a potent PROTAC K-Ras degrader that demonstrates a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T18055 |
K-Ras ligand-Linker Conjugate 2
|
Others | Others |
K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker. This compound is capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC K-Ras Degrader-1, which is a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T18059 |
K-Ras ligand-Linker Conjugate 6
|
Others | Others |
K-Ras ligand-Linker Conjugate 6 is a chemical compound that combines a ligand for K-Ras recruiting moiety and a PROTAC linker. This compound can recruit E3 ligases, including VHL, CRBN, MDM2, and IAP. K-Ras ligand-Linker Conjugate 6 is particularly useful in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1]. | |||
T18058 |
K-Ras ligand-Linker Conjugate 5
|
Others | Others |
K-Ras ligand-Linker Conjugate 5 is a chemical compound that combines a ligand for the K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The K-Ras ligand-Linker Conjugate 5 plays a crucial role in the synthesis of PROTAC K-Ras Degrader-1, a highly potent K-Ras degrader. In SW1573 cells, this degrader exhibits an impressive degradation efficacy of ≥70% [1]. | |||
T18054 | K-Ras ligand-Linker Conjugate 1 | Others | Others |
K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1]. | |||
T18853 |
Tos-PEG4-THP
|
Others | Others |
Tos-PEG4-THP is a polyethylene glycol (PEG) derivative utilized as a linker in the synthesis of PROTAC K-Ras Degrader-1, a potential therapeutic compound for targeted degradation of K-Ras protein [1]. | |||
T18057 |
K-Ras ligand-Linker Conjugate 4
|
Others | Others |
K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T76215 |
KRpep-2d
|
||
KRpep-2d 是一种有效的 K-Ras 抑制剂,抑制 K-Ras 驱动的癌细胞增殖。KRpep-2d 可用于癌症研究。 | |||
T18846 |
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH
|
Others | Others |
THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a polyethylene glycol (PEG) based PROteolysis TArgeting Chimera (PROTAC) linker, employed for the synthesis of PROTAC K-Ras Degrader-1, as documented in reference [1]. | |||
T36391 | Spiro-Oxanthromicin A | ||
Spiro-oxanthromicin A is a polyketide that has been found inStreptomyces.1It induces mislocalization of K-RAS in MDCK cells (IC50= 26.7 μM). 1.Salim, A.A., Xiao, X., Cho, K.J., et al.Rare Streptomyces sp. polyketides as modulators of K-Ras localisationOrg. Biomol. Chem.12(27)4872-4878(2014) | |||
T82136 |
ICMT-IN-1
|
||
ICMT-IN-1 (化合物75) 作为一种高效的ICMT抑制剂展现出显著活性(IC50=0.0013 μM),能够剂量依赖性地在HCT-116细胞中导致ICMT的胞质内积累,进而有效抑制携带K-Ras和N-Ras变异的多个癌细胞系的增殖。 | |||
T82108 | ICMT-IN-35 | ||
ICMT-IN-35(即compound 10n),作为FTPA-triazole类ICMT抑制剂(IC50=0.8 μM),能被哺乳动物细胞吸收并阻断K-Ras膜定位,进而诱导K-Ras错定位。ICMT-IN-35对ICMT+/+MEF细胞表现出选择性细胞毒性,对转移性胰腺癌细胞系展示低微摩尔级别活性(IC50=0.8 μM)。 | |||
T82086 |
ICMT-IN-7
|
||
ICMT-IN-7(化合物74)是一种高效的ICMT抑制剂,其IC50值为0.015 μM。该化合物能剂量依赖性地在HCT-116细胞中诱导ICMT蛋白在胞质的积累,并能抑制表达K-Ras和N-Ras的多种癌细胞系的增殖。 | |||
T74973 | KRas G12R inhibitor 1 | ||
KRas G12R inhibitor 1 (compound 3) 是一种 KRas G12R 选择性共价抑制剂,可以利用突变半胱氨酸的强亲核性,在 K-Ras 的 Switch II 区域不可逆结合。KRas G12R inhibitor 1 可用于癌症研究。 | |||
T79464 |
RORγ antagonist 1
|
ROR | Metabolism |
RORγ antagonist1 (化合物22) 作为RORγ的有效拮抗剂 (KD=0.18 μM),在HPAF-II胰腺癌异种移植模型中显示出了抗增殖性能。该化合物通过抑制RAS/MAPK和AKT/mTORC1通路,并引发caspase依赖的细胞凋亡(apoptosis)机制,从而在胰腺癌细胞中发挥作用。 | |||
T73822 | GGTI-286 TFA | ||
GGTI-286 TFA 是一种高效的细胞通透性 GGTase I 抑制剂,(IC50为 2 μM。在 NIH3T3 细胞中,GGTI-286 TFA 对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50s=2 和 >30 μM)。GGTI-286 TFA 还能有效抑制 K-Ras4B 刺激,IC50为 1 μM。 | |||
T62379 |
GGTI-286
|
||
GGTI-286 是一种高效的、具有细胞通透性 GGTase I 抑制剂 (IC50: 2 μM)。GGTI-286 对 NIH3T3 细胞中的 Rap1A 香叶香叶基化的(IC50: 2 μM)抑制作用强于 H-Ras 的法尼化作用(IC50>30 μM)。GGTI-286 也可以有效抑制 K-Ras4B 刺激(IC50: 1 μM)。 | |||
T62980 | GGTI-286 hydrochloride | ||
GGTI-286 hydrochloride 是一种 GGTase I 的高效抑制剂 (IC50: 2 μM),也能够有效抑制 K-Ras4B (IC50: 1 μM)。GGTI-286 hydrochloride 在 NIH3T3 细胞中,对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50=2和 >30 μM)。 |