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

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.

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IHCH-3185

IHCH-3185 Chemical Structure

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IHCH-3185 Related Antibodies

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

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Description

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)

In Vitro

IHCH-3185 (compound 13t) inhibits recombinant human HDAC1 (IC50=102.9 nM, 15 min), exerts moderate inhibitory effects on HDAC2 and HDAC3, and shows no inhibitory activity against HDAC4 or HDAC6 even at concentrations up to 10 μM[1].
IHCH-3185 inhibits the human A2AR receptor-mediated cAMP signaling pathway in HEK293-A2 AR cells, with an IC50 of 88 nM[1].
IHCH-3185 exhibits broad-spectrum antiproliferative activity in a variety of human and mouse tumor cell lines, with a GI50 ranging from 0.06 μM (DoHH2) to 1.8 μM (MC38, SK-BR-3)[1].
IHCH-3185 (0.3-3.0 μM; 48 h) induces G0/G1 phase arrest in a concentration-dependent manner in murine colon cancer cell lines CT26 and HCT-116 following treatment at concentrations of 0.3, 1.0 and 3.0 μM for 48 h[1].
IHCH-3185 (1.5 nM; 72 h) reverses the inhibitory effect of NECA on IFN-γ secretion in activated mouse splenocytes, with an incubation time of 72 h[1].
IHCH-3185 (0.3-3.0 μM; 24 h) induces concentration-dependent increases in the levels of acetylated histone H3 and H4 in CT26 and MC38 mouse colon cancer cells following treatment at 0.3, 1.0 and 3.0 μM for 24 h[1].
IHCH-3185 (1-10 μM; 24 h) upregulates the mRNA expression of H2-K1, Cxcl9 and Cxcl10 in MC38 mouse colon cancer cells in a concentration-dependent manner after 24 h of treatment at 1, 3 and 10 μM[1].

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

IHCH-3185 Related Antibodies

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.
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 % / /
In Vivo

IHCH-3185 (compound 13t) (120 mg/kg; p.o.; once daily; for 14 consecutive days) exhibits a tumor regression efficiency of 71.1% in a mouse model of MC38[1].

MedChemExpress (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.
Molecular Weight

455.47

Formula

C24H21N7O3
SMILES

NC1=NC(OCCC2=CC=C(C=C2)C(NC3=CC=CC=C3N)=O)=CC4=NC(C5=CC=CO5)=NN41
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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IHCH-3185 Related Classifications

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Help & FAQs
  • 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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