2. Cell Cycle/DNA Damage Epigenetics GPCR/G Protein
  3. HDAC Adenosine Receptor
  4. IHCH-3185

IHCH-3185 是一种口服有效的 I 类 HDAC 抑制剂 (HDAC1 IC50=102.9 nM) 和 A2AR 拮抗剂 (A2AR Ki =7.6 nM)。IHCH-3185 能通过诱导组蛋白乙酰化逆转免疫基因沉默，并阻断腺苷信号通路以解除对 T 细胞的抑制。IHCH-3185 具有抗增殖活性、诱导细胞周期期阻滞的同时，还能显著改善肿瘤微环境。IHCH-3185 降低调节性 T 细胞比例、提高 CD8+/Treg 比值以及上调 H2-K1、Cxcl9 和 Cxcl10 等关键因子的表达。IHCH-3185 在 CT26 和 MC38 小鼠肿瘤模型中展现出显著的抗肿瘤潜力，适用于相关癌症研究。

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IHCH-3185

IHCH-3185 Chemical Structure

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IHCH-3185 相关抗体

Top Publications Citing Use of Products

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IHCH-3185 is an orally active class I HDAC inhibitor (HDAC1 IC50 =102.9 nM) and A2AR antagonist (A2AR Ki =7.6 nM). IHCH-3185 reverses immune gene silencing by inducing histone acetylation and blocks the adenosine signaling pathway to relieve T-cell suppression. IHCH-3185 exhibits antiproliferative activity, induces cell cycle arrest, and significantly improves the tumor microenvironment. IHCH-3185 reduces the proportion of regulatory T cells, increases the CD8+/Treg ratio, and upregulates the expression of key factors such as H2-K1, Cxcl9 and Cxcl10. IHCH-3185 shows significant antitumor potential in CT26 and MC38 mouse tumor models and is suitable for related cancer research[1].
IC50 & Target

HDAC1

102.9 nM (IC50)

A2AR

7.6 nM (Ki)

体外研究
(In Vitro)

IHCH-3185 (compound 13t) 抑制重组人源 HDAC1 (IC50=102.9 nM, 15 min)，对 HDAC2 和 HDAC3 具有中等抑制作用，且在浓度高达 10 μM 时对 HDAC4 或 HDAC6 无抑制活性[1]。
IHCH-3185 在 HEK293-A2AR 细胞中抑制人源 A2AR 受体介导的 cAMP 信号通路， IC50 为 88 nM[1]。
IHCH-3185 在多种人和小鼠肿瘤细胞系中表现出广谱抗增殖活性，GI50 为 0.06 μM (DoHH2) 至 1.8 μM (MC38、SK-BR-3)[1]。
IHCH-3185 (0.3-3.0 μM; 48 h) 可在 0.3、1.0 和 3.0 μM 浓度处理 48 小时后，以浓度依赖方式诱导 CT26 和 HCT-116 小鼠结肠癌细胞发生 G0/G1 期阻滞[1]。
IHCH-3185 (1.5 nM; 72 h) 可逆转 NECA 对活化小鼠脾细胞中 IFN-γ 分泌的抑制作用，孵育时间为 72 小时[1]。
IHCH-3185 (0.3-3.0 μM; 24 h) 可在 0.3、1.0 和 3.0 μM 处理 24 h 后，在 CT26 和 MC38 小鼠结肠癌细胞中诱导乙酰化组蛋白 H3 和 H4 水平呈浓度依赖性升高[1]。
IHCH-3185 (1-10 μM; 24 h) 可在 1、3 和 10 μM 处理 24 小时后，以浓度依赖方式上调 MC38 小鼠结肠癌细胞中 H2-K1、Cxcl9 和 Cxcl10 的 mRNA 表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IHCH-3185 相关抗体:

Cell Viability Assay[1]

Cell Line: CT26, MC38, GP-2d, SW620, HCT-116, T-47D, SK-BR-3, NCI-H1975, PC-9, SU-DHL-4, DoHH2
Concentration: 0.00005-10 μM
Incubation Time: 72 h
Result: Exhibited broad-spectrum antiproliferative activity with GI50 values of 0.38 μM (CT26), 1.8 μM (MC38), 0.6 μM (GP-2d), 0.6 μM (SW620), 0.2 μM (HCT-116), 0.8 μM (T-47D), 1.8 μM (SK-BR-3), 0.5 μM (NCI-H1975), 0.4 μM (PC-9), 0.5 μM (SU-DHL-4), and 0.06 μM (DoHH2).

Cell Cycle Analysis[1]

Cell Line: CT26, HCT-116 mouse colon cancer cell lines
Concentration: 0.3, 1.0, 3.0 μM
Incubation Time: 48 h
Result: Induced a concentration-dependent G0/G1 phase arrest in both CT26 and HCT-116 cells, with significant increases in G0/G1 population and corresponding decreases in S phase population at all tested concentrations.

Western Blot Analysis[1]

Cell Line: CT26, MC38 mouse colon cancer cells
Concentration: 0.3, 1.0, 3.0 μM
Incubation Time: 24 h
Result: Induced a concentration-dependent increase in acetylated H3 and H4 levels in both CT26 and MC38 cells, confirming functional HDAC inhibition.

Real Time qPCR[1]

Cell Line: MC38 mouse colon cancer cells
Concentration: 1-10 μM
Incubation Time: 24 h
Result: Significantly upregulated mRNA expression of H2-K1 (MHC-I), Cxcl9, and Cxcl10 in a concentration-dependent manner, with fold changes relative to vehicle control of ~2.5 (1 μM), ~3 (3 μM), and ~2.8 (10 μM) for H2-K1; ~2 (1 μM), ~4 (3 μM), and ~2.8 (10 μM) for Cxcl9; and ~2 (1 μM), ~4 (3 μM), and ~2.8 (10 μM) for Cxcl10.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2β Tmax Cmax AUC0-t AUC0-∞ MRT F CL Vdss
Mice[1] 5 mg/kg i.v. 1.03 h / 6279 ng/mL 5474 ng·h/mL 5511 ng·h/mL 0.966 h / 15.2 mL/min/kg 0.881 L/kg
Mice[1] 20 mg/kg p.o. 4.29 h 0.667 h 6911 ng/mL 18605 ng·h/mL 18808 ng·h/mL 3.36 h 85 % / /
Mice[1] 100 mg/kg p.o. 6.33 h 0.833 h 38617 ng/mL 134817 ng·h/mL 139094 ng·h/mL 4.48 h 126 % / /
体内研究
(In Vivo)

IHCH-3185 (compound 13t) (120 mg/kg；灌胃；每日 1 次；连续 14 天) 在 MC38 的小鼠模型中表现出 71.1% 的肿瘤消退效率[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (male); BALB/c[1]
Dosage: 60-120 mg/kg (MC38 model); 90-120 mg/kg (CT26 model); 20 mg/kg (PK); 100 mg/kg (PK); 5 mg/kg (PK, IV)
Administration: p.o.; qd; 14 days (antitumor efficacy); p.o. (PK, 20 mg/kg, 100 mg/kg); i.v. (PK, 5 mg/kg)
Result: Achieved TGI of 47.1% (P < 0.05) at 60 mg/kg, 62.2% (P < 0.01) at 90 mg/kg, and 71.1% (P < 0.001) at 120 mg/kg in MC38 syngeneic model.
Achieved TGI of 50.9% (P < 0.01) at 90 mg/kg and 68.5% (P < 0.001) at 120 mg/kg in CT26 syngeneic model.
Showed high oral bioavailability of 85% at 20 mg/kg and 126% at 100 mg/kg in male C57BL/6 mice.
Reduced intratumoral regulatory T-cell populations and increased the CD8+ T-cell/Treg ratio in both CT26 and MC38 models.
Induced histone H3 acetylation in CT26 and MC38 tumor tissues.
Caused no significant body weight loss at all tested doses.
分子量

455.47

Formula

C24H21N7O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

IHCH-3185 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IHCH-3185IHCH3185IHCH 3185HDACAdenosine ReceptorHistone deacetylasesP1 receptorCxcl10regulatory T cellCD8+/Treg ratioA2ARCT26H2-K1T cellCxcl9MC38HDAC1Inhibitorinhibitorinhibit

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IHCH-3185
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