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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
95% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 hydrochloride |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
Lys05 | ✔ | 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 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
LDN-193189 dihydrochloride |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
Alantolactone | ✔ | 98% | |||||||||||||||||
SIS3 | ✔ | 97% | |||||||||||||||||
Pirfenidone | ✔ | 98% | |||||||||||||||||
Hesperetin | ✔ | 97% | |||||||||||||||||
RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
99% | |||||||||||||||||
SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
SB 431542 |
+
ALK5, IC50: 94 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 | Abl ↓ ↑ | Bcr-Abl ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
NVP-BHG 712 |
+
c-Abl, IC50: 1.667 μM |
99%+ | |||||||||||||||||
KW-2449 |
+++
Abl (T315I), IC50: 4 nM Abl, IC50: 14 nM |
FLT3 | 99%+ | ||||||||||||||||
Ponatinib |
++++
Abl, IC50: 0.37 nM |
98% | |||||||||||||||||
AT9283 | 99%+ | ||||||||||||||||||
Imatinib Mesylate |
+
v-Abl, IC50: 600 nM |
PDGFR,c-Kit | 99% | ||||||||||||||||
Danusertib |
++
Abl, IC50: 25 nM |
RET | 99%+ | ||||||||||||||||
Rebastinib |
++++
u-Abl1 (T315I), IC50: 5 nM p-Abl1 (native), IC50: 0.75 nM |
Tie-2,FLT3 | 99%+ | ||||||||||||||||
PP121 |
++
Abl, IC50: 18 nM |
VEGFR,PDGFR | 99%+ | ||||||||||||||||
GNF-7 |
+++
M351T, IC50: 133 nM E255V, IC50: 122 nM |
99%+ | |||||||||||||||||
Olverembatinib dimesylate |
++++
Abl (G250E), IC50: 0.35 nM Abl, IC50: 0.34 nM |
99% | |||||||||||||||||
Dasatinib monohydrate |
++++
Abl , IC50: 0.6 nM |
Src | 98% | ||||||||||||||||
Dasatinib |
++++
Abl, IC50: 0.6 nM |
Src | 98% | ||||||||||||||||
Bafetinib |
+++
Abl, IC50: 5.8 nM |
98+% | |||||||||||||||||
GNF-2 |
+
Bcr-Abl (K562 cell line), IC50: 273 nM Bcr-Abl (SUP-B15 cell line), IC50: 268 nM |
98%+ | |||||||||||||||||
Degrasyn |
+
Bcr-Abl, IC50: 1.8 μM |
DUB | 98+% | ||||||||||||||||
GNF-5 |
++
Bcr-Abl, IC50: 220 nM |
99% | |||||||||||||||||
Radotinib |
++
BCR-ABL1, IC50: 34 nM |
98+% | |||||||||||||||||
PD173955 | Src | 99%+ | |||||||||||||||||
Nilotinib |
++
Bcr-Abl, IC50: <30 nM |
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 | Microtubules, part of the cytoskeleton that provides structure and shape to the cytoplasm of cells, are tubular polymers of tubulin formed by polymerization. Nocodazole is a standard anti-microtubule agent that interferes with the polymerization and now be mostly used as depolymerizing drug in basic cell biology research[8]. Nocodazole can be used as a high-affinity ligand for the cancer-related kinases including Abl phosphorylated, c-Kit, BRAF, and MEK. Furthermore, Nocodazole induces apoptosis in chronic lymphocytic leukemia cells, inhibits insulin-stimulated glucose transport and decreases apoptosis in some human colon carcinoma cells[9]. In vitro Tubulin Polymerization Assays, Nocodazole inhibited tumor cell lines including NCIH460, SKOV3, BT549,451LU, COLO-205 at 48h with IC50 values 68nM, 80nM, 69nM, 72nM, 88nM respectively, which was reflected by a decreased level of steady state turbidity in a dose-dependent manner[5]. To learn how the spindle assembly checkpoint (SAC) inhibitory is extinguished, 9A-Hec1-expressing cells exhibited a robust mitotic arrest after incubation in 5 mM nocodazole for 5 h. As comparison, WT-Hec1 was treated with a moderately low dose (300 nM) of nocodazole, which resulted in the loss of all non-kinetochore spindle microtubules but retention of kinetochore–microtubule[6]. In addition, nocodazole can also improve the CRISPR-mediated HDR efficiency, a 600-bp homology in both arms leads to high-level genome knock in, with 97–100% of the donor insertion events being mediated by HDR. The combined use of CCND1, a cyclin that functions in G1/S transition, and nocodazole, a G2/M phase synchronizer, doubles HDR efficiency to up to 30% in iPSCs, the results showed an additive effect on enhancing precise genome editing[7]. |
作用机制 | Nocodazole will bind to β-Tb and block polymerization, arrest mammalian cells in mitosis and release them into cytokinesis and G1 as well as mis-regulate mitotic kinases[8]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
human 451LU cells | Proliferation assay | 48 h | Antiproliferative activity against human 451LU cells after 48 hrs by alamar blue assay, IC50=72 nM | 21563750 | |
human A549 cells | Proliferation assay | 48 h | Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50=20 nM | 25827522 | |
human A549 cells | Cytotoxic assay | 24 h | Cytotoxicity against human A549 cells after 24 hrs by MTT assay, IC50=36.6 nM | 20110137 | |
human A549 cells | Growth inhibition assay | Growth inhibition of human A549 cells by Sulforhodamine B assay, GI50=0.1 μM | 21106458 | ||
Dose | Mice: 15 mg/kg - 60 mg/kg[3] (i.p.), 5 mg/kg[4] (i.p.) |
Administration | i.p. |
[1]7(1):53-6. doi: 10.1002/cmdc.201100410. Epub 2011 Oct 14.
[2]7(1):53-6. doi: 10.1002/cmdc.201100410. Epub 2011 Oct 14.
[3]54(12):4247-63. doi: 10.1021/jm200436t. Epub 2011 May 26.
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.32mL 0.66mL 0.33mL |
16.59mL 3.32mL 1.66mL |
33.19mL 6.64mL 3.32mL |
CAS号 | 31430-18-9 |
分子式 | C14H11N3O3S |
分子量 | 301.32 |
别名 | Oncodazole;R17934;NSC238159 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
溶解方案 |
DMSO: 18 mg/mL(59.74 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 |
IP 2% DMSO+2% Tween80+30% PEG300+water 0.4 mg/mL clear PO 0.5% CMC-Na 65 mg/mL suspension |