MedKoo Cat#: 525696 | Name: CLK-IN-T3 HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

MDK-5561, also known as CLK-IN-T3, is a novel highly selective, stable CLK inhibitor with high specificity to CLK1-3 protein isoforms. CLK-IN-T3 (MDK-5561) has CAS#2109805-56-1. The last 4 digits of the CAS# is used for name for the convenience of scientific communications. T3-CLK is a pan-CLK inhibitor, T3-CLK as well as the negative control T3-CLK-N have been developed in collaboration with Takeda 3 (5). T3-CLK is a potent inhibitor of CLK1, CLK2 and CLK3 with IC50 of 0.67/15/110 nM, respectively. T3-CLK is >30 fold selective against the closest off targets DYRK1A and DYRK1B with an IC50 of 260 nM and 230 nM, respectively in cellular assays. T3-CLK is non-toxic in cells and inhibits the phosphorylation of SRSF in HeLa cells in a time and dose dependent manner. (https://www.thesgc.org/chemical-probes/T3-CLK)

Chemical Structure

CLK-IN-T3 HCl
CAS#CLK-IN-T3 HCl

Theoretical Analysis

MedKoo Cat#: 525696

Name: CLK-IN-T3 HCl

CAS#: CLK-IN-T3 HCl

Chemical Formula: C28H31ClN6O2

Exact Mass: 0.0000

Molecular Weight: 519.05

Elemental Analysis: C, 64.79; H, 6.02; Cl, 6.83; N, 16.19; O, 6.16

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
T3, CLK Inhibitor T3; T3-CLK; MDK-5561; MDK 5561; MDK5561; MDK-5561 HCl; MDK-5561 hydrochloride
IUPAC/Chemical Name
4-(2-Methyl-1-(4-methylpiperazin-1-yl)-1-oxopropan-2-yl)-N-(6-(pyridin-4-yl)imidazo[1,2-a]pyridin-2-yl)benzamide hydrochloride
InChi Key
KNLKCRDVVPNTAF-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H30N6O2.ClH/c1-28(2,27(36)33-16-14-32(3)15-17-33)23-7-4-21(5-8-23)26(35)31-24-19-34-18-22(6-9-25(34)30-24)20-10-12-29-13-11-20;/h4-13,18-19H,14-17H2,1-3H3,(H,31,35);1H
SMILES Code
O=C(NC1=CN2C=C(C3=CC=NC=C3)C=CC2=N1)C4=CC=C(C(C)(C)C(N5CCN(C)CC5)=O)C=C4.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
The Cdc2-like kinases (CLK) are evolutionary highly conserved dual specificity protein kinases. The CLK family consists of four members, namely CLK1, 2, 3, and 4 (1). CLKs have a highly conserved domain structure at the C-terminus, containing a signature amino acid motif EHLAMMERILG, why they are often referred to as ‘LAMMER kinases’ (2). CLKs auto-phosphorylate on serine/threonine and tyrosine residues and phosphorylate exogenous substrates on serine/threonine residues (3). They play an important role in the regulation of RNA splicing through phosphorylation of members of the serine and arginine-rich family of splicing factors (SRSF). Phosphorylation of SRSF on numerous serine residues is a prerequisite for entry of SRSF into the nucleus and for the assembly of the spliceosome (4). Being part of the splicing machinery, CLKs are often associated with the development of many pathologies, including cancer and neurodegenerative disorders. However, to date CLK-dependent RNA processing events remains poorly defined

Preparing Stock Solutions

The following data is based on the product molecular weight 519.05 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL