Butyzamide是一种口服有效的 Mpl 激活剂,Mpl 是血小板生成素受体。Butyzamide 增加 JAK2、STAT3、STAT5 和 MAPK 的磷酸化水平,并在小鼠异种移植实验中提升人血小板水平。
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产品名称 | JAK1 ↓ ↑ | JAK2 ↓ ↑ | JAK3 ↓ ↑ | Tyk2 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Decernotinib |
+++
JAK1, IC50: 11 nM JAK1, Ki: 11 nM |
+++
JAK2, Ki: 13 nM |
++++
JAK3, Ki: 2.5 nM |
+++
TYK2, Ki: 13 nM |
99%+ | ||||||||||||||
ZM39923 HCl |
+
JAK1, pIC50: 4.4 |
+
JAK3, pIC50: 7.1 |
EGFR | 97% | |||||||||||||||
Cerdulatinib |
+++
JAK1, IC50: 12 nM |
+++
JAK2, IC50: 6 nM |
+++
JAK3, IC50: 8 nM |
++++
TYK2, IC50: 0.5 nM |
99%+ | ||||||||||||||
Momelotinib |
+++
JAK1, IC50: 11 nM |
++
JAK2, IC50: 18 nM |
+
JAK3, IC50: 155 nM |
99%+ | |||||||||||||||
XL019 |
+
JAK1, IC50: 134.3 nM |
++++
JAK2, IC50: 2.2 nM |
+
JAK3, IC50: 214.2 nM |
FLT3 | 99%+ | ||||||||||||||
Ruxolitinib |
+++
JAK1, IC50: 3.3 nM |
++++
JAK2, IC50: 2.8 nM |
98% | ||||||||||||||||
Tofacitinib |
+
JAK1, IC50: 112 nM |
++
JAK2, IC50: 20 nM |
++++
JAK3, IC50: 1 nM |
98% | |||||||||||||||
Ruxolitinib (S enantiomer) |
+++
JAK1, IC50: 3.3 nM |
++++
JAK2, IC50: 2.8 nM |
++
TYK2, IC50: 19 nM |
98% | |||||||||||||||
Filgotinib |
+++
JAK1, IC50: 10 nM |
++
JAK2, IC50: 28 nM |
+
JAK3, IC50: 810 nM |
+
TYK2, IC50: 116 nM |
99% | ||||||||||||||
Baricitinib |
+++
JAK1, IC50: 5.9 nM |
+++
JAK2, IC50: 5.7 nM |
++
TYK2, IC50: 53 nM |
99% | |||||||||||||||
Gandotinib |
++
JAK1, IC50: 19.8 nM |
++++
JAK2, IC50: 0.288 nM JAK2 (V617F), Ki: 0.245 nM |
++
JAK3, IC50: 48.0 nM |
++
TYK2, IC50: 44 nM |
FLT3 | 99%+ | |||||||||||||
Oclacitinib maleate |
+++
JAK1, IC50: 10nM |
++
JAK2, IC50: 18nM |
+
JAK3, IC50: 99nM |
+
TYK2, IC50: 84nM |
98+% | ||||||||||||||
NVP-BSK805 2HCl |
++
JAK1, IC50: 31.63 nM |
++++
JAK2, IC50: ~0.5 nM |
++
JAK3, IC50: 18.68 nM |
+++
TYK2, IC50: 10.76 nM |
99+% | ||||||||||||||
Peficitinib | ✔ | 98% | |||||||||||||||||
Go6976 | ✔ | FLT3 | 99%+ | ||||||||||||||||
AZD-1480 |
++++
JAK2, IC50: 0.26 nM |
99%+ | |||||||||||||||||
Fedratinib |
+++
JAK2, IC50: 3 nM JAK2 (V617F), IC50: 3 nM |
RET,FLT3 | 99%+ | ||||||||||||||||
WP1066 |
+
JAK2, IC50: 2.3 μM |
98% | |||||||||||||||||
Curcumol | ✔ | 98% | |||||||||||||||||
AZ960 |
++++
JAK2, IC50: <3 nM JAK2, Ki: 0.45 nM |
97% | |||||||||||||||||
GLPG0634 analog | ✔ | 99%+ | |||||||||||||||||
CEP-33779 |
++++
JAK2, IC50: 1.8 nM |
99%+ | |||||||||||||||||
FLLL32 |
+
JAK2, IC50: <5 μM |
99%+ | |||||||||||||||||
WHI-P154 |
+
JAK3, IC50: 1.8 μM |
Src,EGFR,VEGFR | 98% | ||||||||||||||||
BMS-911543 |
++++
JAK2, IC50: 1.1 nM |
+
JAK3, IC50: 75 nM |
++
TYK2, IC50: 66 nM |
98% | |||||||||||||||
TG101209 |
+++
JAK2, IC50: 6 nM |
+
JAK3, IC50: 169 nM |
RET,FLT3 | 99%+ | |||||||||||||||
AT9283 |
++++
JAK2, IC50: 1.2 nM |
++++
JAK3, IC50: 1.1 nM |
99%+ | ||||||||||||||||
Pacritinib |
++
JAK2, IC50: 23 nM JAK2 (V617F), IC50: 19 nM |
+
JAK3, IC50: 520 nM |
++
TYK2, IC50: 50 nM |
FLT3 | 97% | ||||||||||||||
Tofacitinib citrate |
++
JAK2, IC50: 20 nM |
++++
JAK3, IC50: 1 nM |
99% | ||||||||||||||||
FM-381 |
++++
JAK3, IC50: 127 pM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | STAT1 ↓ ↑ | STAT3 ↓ ↑ | STAT5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Nifuroxazide | ✔ | 98% | |||||||||||||||||
Fludarabine | ✔ | 98% | |||||||||||||||||
Artesunate | ✔ | 98% | |||||||||||||||||
BP-1-102 |
+++
STAT3, Kd: 504 nM |
99%+ | |||||||||||||||||
Niclosamide |
++
STAT3, IC50: 0.7 μM |
98% | |||||||||||||||||
Napabucasin | ✔ | 98% | |||||||||||||||||
Cryptotanshinone |
++
STAT3, IC50: 4.6 μM |
98% | |||||||||||||||||
Stattic |
+
STAT3, IC50: 5.1 μM |
98% | |||||||||||||||||
NSC 74859 |
+
STAT3, IC50: 86 μM |
99%+ | |||||||||||||||||
Ochromycinone | ✔ | 98% | |||||||||||||||||
HO-3867 | ✔ | 97% | |||||||||||||||||
C188-9 |
++++
STAT3, Kd: 4.7 nM |
99%+ | |||||||||||||||||
HJC0152 | ✔ | 98% | |||||||||||||||||
SH5-07 | ✔ | 97% | |||||||||||||||||
SH-4-54 |
++++
STAT3, Kd: 300 nM |
+++
STAT5, Kd: 464 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
98% | |||||||||||||||||
SB 203580 | 99%+ | ||||||||||||||||||
Pexmetinib | ✔ | Tie-2 | 99%+ | ||||||||||||||||
Skepinone-L |
++++
p38α, IC50: 5 nM |
98% | |||||||||||||||||
Doramapimod |
++++
p38α, Kd: 0.1 nM p38α, IC50: 38 nM |
99%+ | |||||||||||||||||
VX-702 | 99%+ | ||||||||||||||||||
Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
98% | |||||||||||||||||
SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
99%+ | ||||||||||||||||
Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
99%+ | ||||||||||||||||
Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
99%+ | ||||||||||||||||
PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
98% | ||||||||||||||||
TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
99%+ | ||||||||||||||||
SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
99%+ | ||||||||||||||||
Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
98%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Butyzamide is an orally bioavailable stimulator of Mpl, a thrombopoietin (TPO) receptor. It enhances the phosphorylation of JAK2, STAT3, STAT5, and MAPK. Additionally, Butyzamide elevates human platelet levels in a mouse xenotransplantation assay[1]. |
体内研究 | Butyzamide (10 mg/kg, 50 mg/kg; oral administration; once daily for 20 days) elevates human platelet levels in NOG mice transplanted with human fetal liver-derived CD34+ cells[1]. |
体外研究 | In Ba/F3-hMpl cells, treatment with Butyzamide (3 μM; 15 min) triggers the phosphorylation of JAK2, STAT3, STAT5, and MAPK[1]. Butyzamide (3 μM; 48 h) stimulates the formation of colony-forming unit-megakaryocyte and polyploid megakaryocytes from human CD34+ hematopoietic progenitor cells[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.69mL 0.34mL 0.17mL |
8.45mL 1.69mL 0.85mL |
16.90mL 3.38mL 1.69mL |
CAS号 | 1110767-45-7 |
分子式 | C29H32Cl2N2O5S |
分子量 | 591.546 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(177.5 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |