Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11708 |
JAK2-IN-4
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK2-IN-4 is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively. | |||
T2638 |
Gandotinib
LY2784544 |
VEGFR; FGFR; FLT; JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Gandotinib (LY2784544) 是一种JAK2抑制剂,IC50为 3 nM。它也抑制FLT3、FLT4、FGFR2、TYK2 和 TRKB,IC50分别为 4、25、32、44 和 95 nM。 | |||
T11707 | JAK2/FLT3-IN-1 | JNK | MAPK |
JAK2/FLT3-IN-1 has anti-cancer activity. JAK2/FLT3-IN-1 is a potent and orally effective dual JAK2/FLT3 (Janus kinase 2/ FMS-like tyrosine kinase 3) inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. | |||
T15606 |
JAK1-IN-4
|
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK1-IN-4 is a selective JAK1 inhibitor (IC50s: 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively). JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). | |||
T64104 | JAK2/FLT3-IN-1 TFA | ||
JAK2/FLT3-IN-1 (TFA) 是一种口服具有活力的 JAK2/FLT3 双重抑制剂,表现出抗癌效果,能够作用于 JAK2 (IC50: 0.7 nM),FLT3 (IC50: 4 nM),JAK1 (IC50: 26 nM) 和 JAK3 (IC50: 39 nM)。 | |||
T77944 |
SJ1008030 formic
|
PROTACs | PROTAC |
SJ1008030 formic(化合物8)是一款针对JAK2的PROTAC,能够选择性地降解JAK2。该化合物在抑制MHH-CALL-4细胞系增殖方面表现出5.4 nM的IC50值,适用于白血病的研究。 | |||
T16995 |
TAS05567
|
FLT; c-RET; JAK; Syk | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR, and RET with IC50s of 10 nM, 4.8 nM, 600 nM, and 29 nM, respectively) in a panel of 192 kinases. | |||
T40097 |
RET-IN-4
|
||
RET-IN-4 is a highly effective and specific RET inhibitor that can be administered orally. It demonstrates remarkable potency, with IC50 values of 1.29 nM, 1.97 nM, and 0.99 nM for inhibiting RET variants including RET (WT), RET (V804M), and RET (M918T), respectively. Moreover, RET-IN-4 exhibits superior selectivity towards kinases JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). Additionally, RET-IN-4 possesses pronounced anticancer properties. | |||
T79368 | Antiproliferative agent-34 | EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Antiproliferative agent-34 (Compound A14) 是一种多激酶抑制剂,能有效抑制包括EGFRL858R/T790M在内的特定EGFR基因变异形式,IC50为177 nM,对EGFRWT则为1567 nM。它还能抑制JAK2、ROS1、FLT3、FLT4和PDGFRα的活性,其IC50分别为30.93、106.90、108.00、226.60和42.53 nM。在正常氧气环境中,Antiproliferative agent-34对H1975和HCC827细胞株的抑制IC50值低于40 nM,而在低氧环境下,其抑制效能增强4至6倍,IC50值降至低于10 nM。 | |||
T83866 | LCC-12 formate | ||
LCC-12是一种铜(II)螯合剂,为二甲双胍的衍生物。作为单体,它能结合铜(II)并在20 µM的浓度下减少氢过氧化物依赖的NADH向NAD+的氧化。在10 µM的浓度下,LCC-12降低一次性人类细胞因子激活的单核衍生的巨噬细胞(MDMs)中IL-1β、IL-2、IL-6、IL-8和TNF-α的细胞因子水平,以及JAK2、STAT2和IL-1受体相关激酶4(IRAK4)的水平。此外,同样浓度的LCC-12减少了细胞因子激活的MDMs中CD80+和CD86+的数量。每日0.3 mg/kg的剂量可提高LPS或盲肠结扎穿孔模型小鼠的存活率。 |