2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. KG-655

KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research.

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KG-655

KG-655 Chemical Structure

CAS No. : 349-58-6

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Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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KG-655 Related Antibodies

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Description

KG-655 is a ligand that specifically binds to the ARNT PAS-B domain. KG-655 binds to the internal cavity of ARNT PAS-B to restrict its variable folded conformation, disrupts the interaction between ARNT PAS-B and the transcriptional coactivator TACC3, and promotes the homodimerization of ARNT PAS-B. KG-655 is widely applicable to cancer-related research[1][2].

IC50 & Target[1]

FGFR-TACC3

 

In Vitro

KG-655 (5 μM) promotes homodimerization of the wild-type human ARNT PAS-B domain, though less strongly than KG-548[1].
KG-655 (1 mM) binds to both the β-sheet surface (dependent on residues I364 and I458) and an internal cavity of the wild-type human ARNT PAS-B domain, with the two binding modes acting independently[1].
KG-655 (5 mM) binds to the internal cavity of the ARNT PAS-B ARNTI458V mutant, demonstrating that its internal binding mode is independent of surface binding[1].
KG-655 (5 mM) exhibits millimolar binding affinity to wild-type human ARNT PAS-B via dual surface and internal modes; the Y456T mutation substantially disrupts its surface binding but allows retained, reduced internal cavity binding with high micromolar to low millimolar affinity[1].
KG-655 (5 mM) binds to both the β-sheet surface (via residue I458) and internal cavity of wild-type human ARNT PAS-B, with the two binding modes acting independently as disruption of surface binding does not affect internal binding[1].
KG-655 binds within the internal cavity of the wild-type human ARNT PAS-B domain in multiple orientations, consistent with NOE-based distance restraints and requiring partial opening of the cavity[1].
Binding of KG-655 to human ARNT PAS-B reduces pressure-induced nonlinear 15N chemical shift heterogeneity, with stdev(ci [15N]) decreasing from 84 × (2×10-10 ppm/bar2) to 51 × (2×10-10 ppm/bar2), consistent with internal cavity binding[2].

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

KG-655 Related Antibodies
Molecular Weight

230.11

Formula

C8H4F6O
CAS No.
Appearance

<20°C Solid,>21°C Liquid

Color

Colorless to off-white

SMILES

OC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (869.15 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 4.3457 mL 21.7287 mL 43.4575 mL
5 mM 0.8691 mL 4.3457 mL 8.6915 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (21.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (21.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.87%

SDS (393 KB)

COA (248 KB) HNMR (115 KB) RP-HPLC (235 KB)

Handling Instructions (2659 KB)
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 (stored under nitrogen). 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 4.3457 mL 21.7287 mL 43.4575 mL 108.6437 mL
5 mM 0.8691 mL 4.3457 mL 8.6915 mL 21.7287 mL
10 mM 0.4346 mL 2.1729 mL 4.3457 mL 10.8644 mL
15 mM 0.2897 mL 1.4486 mL 2.8972 mL 7.2429 mL
20 mM 0.2173 mL 1.0864 mL 2.1729 mL 5.4322 mL
25 mM 0.1738 mL 0.8691 mL 1.7383 mL 4.3457 mL
30 mM 0.1449 mL 0.7243 mL 1.4486 mL 3.6215 mL
40 mM 0.1086 mL 0.5432 mL 1.0864 mL 2.7161 mL
50 mM 0.0869 mL 0.4346 mL 0.8691 mL 2.1729 mL
60 mM 0.0724 mL 0.3621 mL 0.7243 mL 1.8107 mL
80 mM 0.0543 mL 0.2716 mL 0.5432 mL 1.3580 mL
100 mM 0.0435 mL 0.2173 mL 0.4346 mL 1.0864 mL
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KG-655 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.

Keywords:

KG-655349-58-6KG655KG 655FGFRFibroblast growth factor receptorβ-sheet surfaceI364I458ARNT PAS-B domaincancerinternal cavityARNT PAS-B I458V mutantTACC3 transcriptional coactivatorhomodimerizationY456T mutationInhibitorinhibitorinhibit

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