k-ras-in-1

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。

pan-KRAS-IN-17 (Example 34) 是一种广谱的KRAS抑制剂。

SOS1 KRAS-IN-1(Compound 2)为针对SOS1 KRAS介导的疾病进行研究而设计的抑制剂。

Pan-KRAS-IN-15 (compound 58) is a pan-KRAS inhibitor used in pancreatic cancer research [1].

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。

K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C.

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].

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].

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].

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].

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].

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].

THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, facilitates the synthesis of PROTAC K-Ras Degrader-1[1].

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].

XMU-MP-9是一款双功能化合物，能够同时与Nedd4-1的C2结构域和Kras的变构位点结合。该化合物通过加强Nedd4-1与K-Ras之间的相互作用，诱导二者复合物的构象改变，进而促进多种K-Ras突变型的泛素化及其随后的降解。此外，XMU-MP-9还能有效抑制带有K-Ras突变的细胞增殖，因此，它在癌症研究领域具有潜在的应用价值。

PROTAC K-Ras Degrader-3（化合物 40）为特定靶向K-Ras的PROTAC降解剂，其在SW620 KRAS G12D 细胞上体现出极高效力，DC50 值不超过1 nM，同时对SW620 3D 细胞生长的GI50 值亦不高于10 nM。该化合物常用于癌症领域的研究工作。

DSPE-PEG(2000) maleimide 作为1,2-二硬脂酰-sn-磷脂醇（DSPE）的PEG化衍生物，广泛应用于体外及体内合成输送siRNA或小分子抗癌药物的脂质纳米粒子（LNPs）。在相关实验中，含有DSPE-PEG(2000) maleimide的LNPs，其封装了针对p53和K-RAS mRNA的siRNA，在PANC-1胰腺导管腺癌小鼠异种移植模型中成功诱导肿瘤退化。

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)

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。

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)。

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)。

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。

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。

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。