1. Cell Cycle/DNA Damage Anti-infection
  2. CDK HIV HSV
  3. LDC4297 hydrochloride

LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection.

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

LDC4297 hydrochloride Chemical Structure

LDC4297 hydrochloride Chemical Structure

CAS No. : 2319747-14-1

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Based on 5 publication(s) in Google Scholar

Other Forms of LDC4297 hydrochloride:

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Description

LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection[1].

IC50 & Target

CDK7

0.13 nM (IC50)

166v VP22-GFP

0.02 μM (EC50)

01-6332

0.27 μM (EC50)

HIV-1 (NL4.3 strain)

1.04 μM (EC50)

4LIG7

1.13 μM (EC50)

In Vitro

LDC4297 hydrochloride (0-10 μM; 6 d) dose-dependently inhibits HCMV replication with an EC50 value of 24.5 nM[1].
LDC4297 hydrochloride (0-10 μM; 4 d) shows anti-proliferative activity to primary cultures of fibroblasts derived from human (HFF) with a GI50 value of 4.5 μM[1].
LDC4297 hydrochloride (20 μM; 12-96 h) shows anti-HCMV activity through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation[1].
LDC4297 hydrochloride (0-10 μM; 7 d) shows broad antiviral activities to HCMV, GPCMV, MCMV, HVV-6A, HSV-1, HSV-2, VZV, EBV, HAdV-2, Vaccinia virus, HIV-1 (nl4-3), HIV-1 (4LIG7) and Influenza A virus with EC50 values of 0.02, 0.05, 0.07, 0.04, 0.02, 0.27, 0.06, 1.21, 0.25, 0.77, 1.04, 1.13 and 0.99 μM, respectively[1].

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

Western Blot Analysis[1]

Cell Line: Primary cultures of fibroblasts derived from human (HFF) with virus infection
Concentration: 20 μM
Incubation Time: 12, 24, 48 and 96 hours
Result: Showed inhibitory effect towards viral protein synthesis at the stage of immediate early (IE) gene expression and the drug-mediated reduction of IE1p72 levels partially recovered over time. Exerted an inhibitory effect on human cytomegalovirus (HCMV) induced an up-regulation of protein expression or protein phosphorylation, and reduced Rb expression in the uninfected control cells at 24 h.
In Vivo

LDC4297 hydrochloride (100 mg/kg; p.o. once) shows promising pharmacokinetic analyses[1].

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

Animal Model: CD1 mice[1]
Dosage: 100 mg/kg
Administration: Oral gavage; 100 mg/kg once
Result: Showed a half-life (t1/2z) of 1.6 h, and the time to a mean peak plasma concentration of 1297.6 ng/mL is reached 0.5 h after administration with a continued presence in plasma for at least 8 h and a bioavailability of 97.7%.
Molecular Weight

468.98

Formula

C23H29ClN8O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)C1=C(N2N=C1)N=C(OC3CNCCC3)N=C2NCC4=CC=CC=C4N5C=CC=N5.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (213.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1323 mL 10.6614 mL 21.3229 mL
5 mM 0.4265 mL 2.1323 mL 4.2646 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1323 mL 10.6614 mL 21.3229 mL 53.3072 mL
5 mM 0.4265 mL 2.1323 mL 4.2646 mL 10.6614 mL
10 mM 0.2132 mL 1.0661 mL 2.1323 mL 5.3307 mL
15 mM 0.1422 mL 0.7108 mL 1.4215 mL 3.5538 mL
20 mM 0.1066 mL 0.5331 mL 1.0661 mL 2.6654 mL
25 mM 0.0853 mL 0.4265 mL 0.8529 mL 2.1323 mL
30 mM 0.0711 mL 0.3554 mL 0.7108 mL 1.7769 mL
40 mM 0.0533 mL 0.2665 mL 0.5331 mL 1.3327 mL
50 mM 0.0426 mL 0.2132 mL 0.4265 mL 1.0661 mL
60 mM 0.0355 mL 0.1777 mL 0.3554 mL 0.8885 mL
80 mM 0.0267 mL 0.1333 mL 0.2665 mL 0.6663 mL
100 mM 0.0213 mL 0.1066 mL 0.2132 mL 0.5331 mL
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LDC4297 hydrochloride Related Classifications

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.

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LDC4297 hydrochloride
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