1. Epigenetics
  2. Histone Demethylase
  3. KDM5-IN-1

KDM5-IN-1 

Cat. No.: HY-100422 Purity: >98.0%
Handling Instructions

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

For research use only. We do not sell to patients.

KDM5-IN-1 Chemical Structure

KDM5-IN-1 Chemical Structure

CAS No. : 1628210-26-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 283 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

KDM5-IN-1 is a potent, selective and orally bioavailable KDM5 inhibitor with an IC50 of 15.1 nM.

IC50 & Target

IC50: 15.1 nM (KDM5); EC50: 0.34 μM (PC9 H3K4Me3)[1]

In Vitro

KDM5-IN-1 is found to potently inhibit KDM5B and KDM5C isoforms (IC50 of 4.7 and 65.5 nM, respectively). It is significantly less potent against other KDM enzymes (1A, 2B, 3B, 4C, 5A, 6A, 7B), inhibiting KDM4C the strongest with an IC50 of 1.9 μM. KDM5-IN-1 still displays more than 100-fold selectivity for KDM4C vs. KDM5A[1].

In Vivo

When dosed orally in mice at 50 mg/kg twice a day, KDM5-IN-1 shows an unbound maximal plasma concentration Cmax>15-fold over its cell EC50, thereby providing a robust chemical probe for studying KDM5 biological functions in vivo[1].

Molecular Weight

324.38

Formula

C₁₇H₂₀N₆O

CAS No.

1628210-26-3

SMILES

N#CC1=C2NC(C3=CN(C(C)(C)C)N=C3)=C(C(C)C)C(N2N=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (92.48 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0828 mL 15.4140 mL 30.8280 mL
5 mM 0.6166 mL 3.0828 mL 6.1656 mL
10 mM 0.3083 mL 1.5414 mL 3.0828 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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KDM5-IN-1
Cat. No.:
HY-100422
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