KDM5A-IN-1 - 99%, high purity , CAS No.1905481-36-8

  • ≥99%
Item Number
K649083
Grouped product items
SKUSizeAvailabilityPrice Qty
K649083-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$150.90
K649083-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$350.90
K649083-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$500.90
K649083-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,500.90
K649083-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$2,100.90
View related series
Epigenetics Histone Demethylase

Basic Description

Specifications & Purity≥99%
Biochemical and Physiological MechanismsKDM5A-IN-1 is a potent, orally bioavailable pan- histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 45 nM, 56 nM and 55 nM for KDM5A , KDM5B and KDM5C , respectively, and with an EC 50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significant
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Product Description

KDM5A-IN-1 is a potent, orally bioavailable pan- histone lysine demethylases 5 (KDM5) inhibitor with IC 50 s of 45 nM, 56 nM and 55 nM for KDM5A , KDM5B and KDM5C , respectively, and with an EC 50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B)

In Vivo

KDM5A-IN-1 (Compound 50, 5 mg/kg; oral administration; female CD-1 mice) treatment shows moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34) and remarkably low plasma protein binding in mice (40%), with t 1/2 of 0.4 hours . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD-1 mice Dosage: 5 mg/kg Administration: Oral administration (Pharmacokinetic study) Result: Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%).

Form:Solid

IC50& Target:IC50: 45 nM ( KDM5A ), 56 nM ( KDM5B ) and 55 nM ( KDM5C )

Associated Targets(Human)

KDM5A Tchem Lysine-specific demethylase 5A (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KDM5C Tchem Lysine-specific demethylase 5C (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KDM5B Tchem Lysine-specific demethylase 5B (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BT-474 (2113 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MCF7 (126967 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SK-BR-3 (5175 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PC-9 (1037 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-231 (73002 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Liver (3974 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM1A Tchem Lysine-specific histone demethylase 1 (3916 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM4C Tchem Lysine-specific demethylase 4C (1129 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PHF8 Tchem Histone lysine demethylase PHF8 (151 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM6A Tchem Lysine-specific demethylase 6A (39 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM5C Tchem Lysine-specific demethylase 5C (224 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM5A Tchem Lysine-specific demethylase 5A (893 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM5B Tchem Lysine-specific demethylase 5B (814 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KDM2B Tchem Lysine-specific demethylase 2B (347 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasma (328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name N-[(3R)-1-(5-propan-2-yl-1H-pyrazole-3-carbonyl)pyrrolidin-3-yl]cyclopropanecarboxamide
INCHI InChI=1S/C15H22N4O2/c1-9(2)12-7-13(18-17-12)15(21)19-6-5-11(8-19)16-14(20)10-3-4-10/h7,9-11H,3-6,8H2,1-2H3,(H,16,20)(H,17,18)/t11-/m1/s1
InChi Key CXEXTVGTDZRKJS-LLVKDONJSA-N
Canonical SMILES CC(C)C1=CC(=NN1)C(=O)N2CCC(C2)NC(=O)C3CC3
Isomeric SMILES CC(C)C1=CC(=NN1)C(=O)N2CC[C@H](C2)NC(=O)C3CC3
PubChem CID 119081409
Molecular Weight 290.36

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Chemical and Physical Properties

SolubilityDMSO : ≥ 50 mg/mL (172.20 mM)

Related Documents

Solution Calculators