ras-in-2

RMC-6236 是一种口服有效、新颖的三复合 RAS(ON)MULTI 抑制剂，是多种 RAS 变体 GTP 结合状态的强效非共价抑制剂。RMC-6236 具有抗肿瘤活性，可用于 RAS 驱动肿瘤的相关研究。凭借在化合物合成方面的丰富经验，我们可以根据您的研究需求为该产品提供快速定制合成服务。

Pan-RAS-IN-2（compound 6A）是一种专门针对RAS分子的靶向胶体(molecular glues)。该化合物能够有效抑制带有RAS突变的细胞系中的细胞增殖。通过与CYPA和RAS(ON)蛋白联合形成三元复合物，Pan-RAS-IN-2阻断了RAS到RAF的信号传递路径，从而发挥其抗肿瘤效果。

Pan-KRAS-IN-2（compound 6）是一种抑制剂，对KRAS WT及其多种突变体（G12D、G12C、G12V、G12S、G12A、Q61H）表现出极高的抑制活性，其IC50均不超过10 nM；然而对KRAS G13D的抑制活性较低，IC50超过10 μM。

UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) 是一种有效的 ICMT 抑制剂，IC50 为 2 μM，对参与 Ras 翻译后修饰的其他酶具有选择性。

Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮，具有较强的抗癌作用。

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。

CHS-111 is a benzyl indazole compound. CHS-111 inhibits superoxide anion (O(2)(-)) generation. CHS-111 reduces the fMLP-stimulated PLD activity (IC(50) 3.9±1.2μM). CHS-111 inhibits the interaction of PLD1 with ADP-ribosylation factor (Arf) 6 and Ras homol

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 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)。

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1 2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB HIF-2α axis[1][2][3].

K-Ras G12C-IN-2 is a covalent kras g12c inhibitor.

PROTACSOS1 degrader-2 是一种有效的 PROTACSOS1降解剂。PROTACSOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTACSOS1degrader-2 在体内显著抑制肿瘤生长。

KRAS G12C inhibitor 69 (Compound K09) 是一种对突变RAS蛋白KRASG12C具备抑制作用的化合物，其IC50值为4.36 nM。它在细胞系NCI-H358和MIA-PACA-2中抑制ERK的磷酸化，IC50值分别为12 nM和7 nM。同时，KRAS G12C inhibitor 69 可以抑制癌细胞NCI-H358和MIA-PACA-2的增殖，其IC50值分别为3.15 nM和2.33 nM。

PAn-RAS-IN-4 (compound 2) 是一种有效抑制RAS的化合物，对KRAS G12D的IC50小于100 nM，在癌症研究中具有重要作用。

Palmostatin B is a modulator of Ras-signaling that acts by targeting acyl protein thioesterase 1 (APT1) and 2 (APT2) in cells.

Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods.

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。

ERK-IN-3 (ASN007 free base) 是一种有效的口服活性 ERK 抑制剂，以低 IC50 值抑制 ERK1 2，可用于研究由 RAS 突变驱动的癌症。

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].

ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK . ERK-IN-3 benzenesulfonate inhibits ERK1 2 with low single-digit nM IC 50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.

MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1 2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (0.006 to 0.2 mM) inhibitory effect on cellular proliferation of H226, MCF-7, U87, LNCaP, A431 and A549 cancer cell lines as determined by in vitro proliferation assays.

PROTAC K-Ras degrader-2 (compound 48) 是一种广谱KRAS突变体PROTAC降解剂，对KRAS G12V RAF1的IC50≤200 nM。该化合物可以降解SW620 KRAS G12D，DC50≤200 nM，并抑制SW620 3D细胞扩增，其IC50≤20 nM。

Pyridostatin TFA 是一种 G-四链体稳定剂，靶向原癌基因 Src，降低人乳腺癌细胞 SRC 蛋白水平和 SRC 依赖的细胞运动。它通过诱导复制和转录依赖的 DNA 损伤促进人类癌细胞生长停滞。

Magnolin 是辛夷的一种主要成分，靶向作用于ERK1和ERK2，IC50值分别为 87 和 16.5 nM，可抑制Ras ERKs RSK2信号通路。它在体内外降低肾脏氧化应激，抑制 caspase-3 活性，并增加 Bcl-2 表达，具有抗炎和抗氧化作用。