Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8756 |
KRAS inhibitor-9
DUN09716 |
Apoptosis; Ras | Apoptosis; GPCR/G Protein; MAPK |
KRAS inhibitor-9 (DUN09716) 是一种 KRAS 抑制剂,阻止 GTP-KRAS 的形成和 KRAS 下游激活。它以中等的结合亲和力与 KRAS G12D、KRAS G12C 和 KRAS Q61H 蛋白结合,选择性抑制具有 KRAS 突变的 NSC-LC 细胞的增殖。它可导致 G2/M 细胞周期停滞并诱导凋亡。 | |||
T12979 |
BI-3406
|
p38 MAPK; MAPK; Ras | GPCR/G Protein; MAPK |
BI-3406 是一种可口服、高效且选择性的 KRAS-SOS1 抑制剂,具有抗癌活性。它有效减少 GTP 加载的 KRAS 的形成,抑制 MAPK 信号通路。它还抑制 KRAS 与 SOS1之间相互作用,IC50为 6 nM。 | |||
T62228 |
KRAS G12D inhibitor 14
|
Ras | GPCR/G Protein; MAPK |
KRAS G12D inhibitor 14 是一种 KRAS G12D 的有效抑制剂,能够结合 KRAS G12D 蛋白 (Kd: 33 nM)。KRAS G12D inhibitor 14 抑制 KRAS G12D (KRAS G12D-GTP) 的活性形式,但对 KRAS G13D 无抑制作用。 | |||
T7414 |
ARS-853
|
Apoptosis; Raf; Ras | Apoptosis; GPCR/G Protein; MAPK |
ARS-853 是一种选择性共价KRAS G12C 抑制剂,IC50为 2.5 μM。它通过与 GDP 结合的癌蛋白结合并阻止激活来抑制突变 KRAS 驱动的信号传导。 | |||
T79213 |
AZD4747
|
Ras | GPCR/G Protein; MAPK |
AZD4747 是一种可透过血脑屏障且具有选择性和有效性的突变GTP酶 KRAS G12C 抑制剂,具有潜在的抗肿瘤活性,可用于研究胰腺癌和结直肠腺癌。 | |||
T38411 |
KRA-533
|
||
KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells. | |||
T63927 | KRAS G12C inhibitor 25 | ||
KRAS G12C inhibitor 25 是 KRAS G12C 抑制剂。KRAS G12C inhibitor 25 能够抑制 KRAS-G12C 突变体的 SOS1 辅助的 GDP/GTP 交换活性,其 IC50 值为 0.48 nM。 | |||
T36642 | RAS/RAS-RAF-IN-1 | ||
RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity[1]. RAS/RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1. |