HPOB是一种高效、选择性的 HDAC6 抑制剂,IC50 为 56 nM,对其他 HDAC 的效力降低了 30 倍以上。HPOB 提高了 DNA 损伤抗癌活性分子在转化细胞中的有效性,但不阻断 HDAC6 的泛素结合活性。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
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Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | HD1 ↓ ↑ | HD2 ↓ ↑ | HDAC ↓ ↑ | HDAC1 ↓ ↑ | HDAC10 ↓ ↑ | HDAC11 ↓ ↑ | HDAC2 ↓ ↑ | HDAC3 ↓ ↑ | HDAC4 ↓ ↑ | HDAC5 ↓ ↑ | HDAC6 ↓ ↑ | HDAC7 ↓ ↑ | HDAC8 ↓ ↑ | HDAC9 ↓ ↑ | 其他靶点 | 纯度 | |||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Givinostat HCl monohydrate |
++++
HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM |
+++
HD2, IC50: 10 nM |
99%+ | ||||||||||||||||
MC1568 |
++
HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM |
96% | |||||||||||||||||
Trichostatin A |
++++
HDAC, IC50: ~1.8 nM |
99%+ | |||||||||||||||||
Scriptaid | ✔ | 99%+ | |||||||||||||||||
Valproic acid sodium | ✔ | Autophagy | 97% | ||||||||||||||||
AR-42 |
+++
HDAC, IC50: 30 nM |
99%+ | |||||||||||||||||
Dacinostat |
+++
HDAC, IC50: 32 nM |
98+% | |||||||||||||||||
CUDC-101 |
++++
HDAC, IC50: 4.4 nM |
++++
HDAC1, IC50: 4.5 nM |
+++
HDAC10, IC50: 26.1 nM |
+++
HDAC2, IC50: 12.6 nM |
++++
HDAC3, IC50: 9.1 nM |
+++
HDAC4, IC50: 13.2 nM |
+++
HDAC5, IC50: 11.4 nM |
++++
HDAC6, IC50: 5.1 nM |
+
HDAC7, IC50: 373 nM |
++
HDAC8, IC50: 79.8 nM |
++
HDAC9, IC50: 67.2 nM |
EGFR,HER2 | 99%+ | ||||||
M344 |
++
HDAC, IC50: 100 nM |
99%+ | |||||||||||||||||
Splitomicin |
+
Sir2p, IC50: 60 μM |
99% | |||||||||||||||||
Panobinostat |
++++
HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM |
98% | |||||||||||||||||
Sodium 4-Phenylbutyrate | ✔ | 98% | |||||||||||||||||
Vorinostat |
+++
HDAC, IC50: ~10 nM |
98% | |||||||||||||||||
Curcumin | ✔ | Nrf2,NF-κB | 98% | ||||||||||||||||
Belinostat |
+++
HDAC, IC50: 27 nM |
98% | |||||||||||||||||
RG-2833 |
++
HDAC1, Ki: 32 nM |
++
HDAC3, Ki: 5 nM |
98% | ||||||||||||||||
Valproic acid |
+
HDAC1, IC50: 0.4 mM |
98% | |||||||||||||||||
BG45 |
+
HDAC1, IC50: 2 μM |
+
HDAC2, IC50: 2.2 μM |
+
HDAC3, IC50: 289 nM |
99%+ | |||||||||||||||
Entinostat |
+
HDAC1, IC50: 0.51 μM |
+
HDAC3, IC50: 1.7 μM |
98% | ||||||||||||||||
Resminostat |
+++
HDAC1, IC50: 42.5 nM |
++
HDAC3, IC50: 50.1 nM |
++
HDAC6, IC50: 71.8 nM |
98+% | |||||||||||||||
Romidepsin |
+++
HDAC1, IC50: 36 nM |
+++
HDAC2, IC50: 47 nM |
99%+ | ||||||||||||||||
Parthenolide | ✔ | p53,NF-κB | 97% HPLC | ||||||||||||||||
Tacedinaline |
+
HDAC1, IC50: 0.9 μM |
+
HDAC2, IC50: 0.9 μM |
+
HDAC3, IC50: 1.2 μM |
98% | |||||||||||||||
Mocetinostat |
++
HDAC1, IC50: 0.15 μM |
+
HDAC11, IC50: 0.59 μM |
+
HDAC2, IC50: 0.29 μM |
+
HDAC3, IC50: 1.66 μM |
98% | ||||||||||||||
WT-161 |
++++
HDAC1, IC50: 8.35 nM |
+++
HDAC2, IC50: 15.4 nM |
++++
HDAC6, IC50: 0.4 nM |
99%+ | |||||||||||||||
Fimepinostat |
++++
HDAC1, IC50: 1.7 nM |
++++
HDAC10, IC50: 2.8 nM |
++++
HDAC11, IC50: 5.4 nM |
++++
HDAC2, IC50: 5.0 nM |
++++
HDAC3, IC50: 1.8 nM |
+++
HDAC6, IC50: 27 nM |
99%+ | ||||||||||||
Tucidinostat |
++
HDAC1, IC50: 95 nM |
++
HDAC10, IC50: 78 nM |
++
HDAC2, IC50: 160 nM |
++
HDAC3, IC50: 67 nM |
99%+ | ||||||||||||||
Santacruzamate A |
++++
HDAC2, IC50: 119 pM |
99%+ | |||||||||||||||||
(E,E)-RGFP966 |
++
HDAC3, IC50: 80 nM |
99%+ | |||||||||||||||||
LMK-235 |
+++
HDAC4, IC50: 11.9 nM |
++++
HDAC5, IC50: 4.2 nM |
99%+ | ||||||||||||||||
Tasquinimod | ✔ | 99%+ | |||||||||||||||||
CAY10603 |
++++
HDAC6, IC50: 2 pM |
98% | |||||||||||||||||
Tubastatin A |
+++
HDAC6, IC50: 15 nM |
98% | |||||||||||||||||
Tubacin |
++++
HDAC6, IC50: 4 nM |
99%+ | |||||||||||||||||
ACY-738 |
++++
HDAC6, IC50: 1.7 nM |
99%+ | |||||||||||||||||
Nexturastat A |
++++
HDAC6, IC50: 5 nM |
99%+ | |||||||||||||||||
BRD73954 |
+++
HDAC6, IC50: 36 nM |
++
HDAC8, IC50: 120 nM |
99% | ||||||||||||||||
Tubastatin A HCl |
+++
HDAC6, IC50: 15 nM |
+
HDAC8, IC50: 854 nM |
98% | ||||||||||||||||
PCI-34051 |
+++
HDAC8, IC50: 10 nM |
99%+ | |||||||||||||||||
Ricolinostat |
++
HDAC1, IC50: 58 nM |
++
HDAC2, IC50: 48 nM |
++
HDAC3, IC50: 51 nM |
++++
HDAC6, IC50: 4.7 nM |
++
HDAC8, IC50: 100 nM |
99%+ | |||||||||||||
Droxinostat |
+
HDAC3, IC50: 16.9 μM |
+
HDAC6, IC50: 2.47 μM |
+
HDAC8, IC50: 1.46 μM |
99%+ | |||||||||||||||
Abexinostat |
++++
HDAC1, Ki: 7 nM |
+++
HDAC10, IC50: 24 nM |
+++
HDAC2, Ki: 19 nM |
++++
HDAC3/SMRT, Ki: 8.2 nM |
+++
HDAC6, Ki: 17 nM |
+
HDAC8, IC50: 280 nM |
98%+ | ||||||||||||
Citarinostat |
+++
HDAC1, IC50: 35 nM |
+++
HDAC2, IC50: 45 nM |
+++
HDAC3, IC50: 46 nM |
++++
HDAC6, IC50: 2.6 nM |
++
HDAC8, IC50: 137 nM |
99%+ | |||||||||||||
HPOB |
+
HDAC1, IC50: 2.9 μM |
+
HDAC10, IC50: 3.0 μM |
+
HDAC2, IC50: 4.4 μM |
+
HDAC3, IC50: 1.7 μM |
++
HDAC6, IC50: 56 nM |
+
HDAC8, IC50: 2.8 μM |
97% | ||||||||||||
Quisinostat 2HCl |
++++
HDAC1, IC50: 0.11 nM |
++++
HDAC10, IC50: 0.46 nM |
++++
HDAC11, IC50: 0.37 nM |
++++
HDAC2, IC50: 0.33 nM |
++++
HDAC3, IC50: 4.86 nM |
++++
HDAC4, IC50: 0.64 nM |
++++
HDAC5, IC50: 3.69 nM |
++++
HDAC8, IC50: 4.26 nM |
99+% | ||||||||||
Domatinostat |
+
HDAC1, IC50: 1.20 μM |
+
HDAC10, IC50: 21 μM |
+
HDAC11, IC50: 9.7 μM |
+
HDAC2, IC50: 1.12 μM |
+
HDAC3, IC50: 0.57 μM |
+
HDAC5, IC50: 11.3 μM |
+
HDAC9, IC50: 50 μM |
99%+ | |||||||||||
TMP269 |
++
HDAC4, IC50: 157 nM |
++
HDAC5, IC50: 97 nM |
+++
HDAC7, IC50: 43 nM |
+++
HDAC9, IC50: 23 nM |
99%+ | ||||||||||||||
Pracinostat |
++
HDAC1, IC50: 49 nM |
+++
HDAC10, IC50: 40 nM |
++
HDAC11, IC50: 93 nM |
++
HDAC2, IC50: 96 nM |
+++
HDAC3, IC50: 43 nM |
++
HDAC4, IC50: 56 nM |
+++
HDAC5, IC50: 47 nM |
+
HDAC6, IC50: 1.008 μM |
++
HDAC7, IC50: 137 nM |
++
HDAC8, IC50: 140 nM |
++
HDAC9, IC50: 70 nM |
99%+ | |||||||
TMP195 |
++
HDAC4, Ki: 59 nM |
++
HDAC5, Ki: 60 nM |
+++
HDAC7, Ki: 26 nM |
+++
HDAC9, Ki: 15 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。 |
靶点 |
|
描述 | HPOB is a selective HDAC6 inhibitor with IC50 value of 56nM, exhibiting at least 30-fold selectivity to HDAC6 over other HDACs. Treatment with HPOB at concentration of 8-32μM for 72h led to cell growth inhibition of normal (HFS) and transformed (LNCaP, A549, and U87) cells but did not induce cell death. HPOB at concentration of 4-16μM caused accumulation of acetylated α-tubulin and acetylated peroxiredoxin, both of which are HDAC6 substrates, in normal (HFS) and transformed (LNCAP, U87, and A549) cells post 24-hour treatment, without effect on acetylated histones. HPOB only inhibited the catalytic activity but not the ubiquitin-binding activity of HDAC6. HPOB had the therapeutic potential in combination therapy to enhance the potency of anticancer drugs including, etoposide, doxorubicin and SAHA in vitro, and enhance anticancer effects of SAHA (50mg/kg) in mice bearing human prostate cancer CWR22 xenograft at dose of 300mg/kg, i.p., for 25 days. |
Dose | Mice: 100 mg/kg - 300 mg/kg[2] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.91mL 3.18mL 1.59mL |
31.81mL 6.36mL 3.18mL |
CAS号 | 1429651-50-2 |
分子式 | C17H18N2O4 |
分子量 | 314.34 |
别名 | |
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,2-8°C |
溶解度 |
DMSO: 50 mg/mL(159.07 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 |