2. PROTAC Cell Cycle/DNA Damage Autophagy Apoptosis Immunology/Inflammation
  3. PROTACs FKBP
  4. KB02-SLF

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.

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KB02-SLF

KB02-SLF 構造式

CAS 番号 : 2384184-40-9

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 522 在庫あり
Solution
10 mM * 1 mL in DMSO USD 522 在庫あり
Solid
5 mg $250 在庫あり
10 mg $400 在庫あり
25 mg $800 在庫あり
50 mg $1280 在庫あり
100 mg $2050 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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KB02-SLF 関連抗体

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製品説明

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF[1].

IC50 & Target[1]

FKBP12

 

体外実験

KB02-SLF (2 μM; 4-72 hours; HEK293T cells) treatment promotes a substantial reduction in nuclear FKBP12 that is sustained across a 4-72 h time frame[1].
Cell imaging studies confirms the selective loss of nuclear-localized FKBP12 in KB02-SLF-treated cells. KB02-SLF promotes the loss of FKBP12_NLS across a concentration of ~0.5-5μM, but shows varied reductions in activity at higher concentrations. The degradation of FKBP12_NLS induced by KB02-SLF is mediated by DCAF16[1].

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

KB02-SLF 関連抗体

Western Blot Analysis[1]

Cell Line: HEK293T cells
Concentration: 2 µM
Incubation Time: 4 hours, 8 hours, 24 hours, 48 hours, 72 hours
Result: Promoted a substantial reduction in nuclear FKBP12 that was sustained across a 4-72 h time frame.
分子量

949.52

分子式

C50H65ClN4O12
CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

O=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@H](C2=CC=CC(NC(CCOCCOCCNC(COC3=CC4=C(N(C(CCl)=O)CCC4)C=C3)=O)=O)=C2)CCC5=CC=C(OC)C(OC)=C5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (105.32 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 1.0532 mL 5.2658 mL 10.5316 mL
5 mM 0.2106 mL 1.0532 mL 2.1063 mL
10 mM 0.1053 mL 0.5266 mL 1.0532 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

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体積 （終了）

V2

体内:

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 5 mg/mL (5.27 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 5 mg/mL (5.27 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 (sealed storage, away from moisture and light)

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.
純度とドキュメンテーション

純度: 99.25%

COA (245 KB) HNMR (785 KB) RP-HPLC (247 KB) LCMS (104 KB)

取扱説明書 (2659 KB)
参考文献

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 1.0532 mL 5.2658 mL 10.5316 mL 26.3291 mL
5 mM 0.2106 mL 1.0532 mL 2.1063 mL 5.2658 mL
10 mM 0.1053 mL 0.5266 mL 1.0532 mL 2.6329 mL
15 mM 0.0702 mL 0.3511 mL 0.7021 mL 1.7553 mL
20 mM 0.0527 mL 0.2633 mL 0.5266 mL 1.3165 mL
25 mM 0.0421 mL 0.2106 mL 0.4213 mL 1.0532 mL
30 mM 0.0351 mL 0.1755 mL 0.3511 mL 0.8776 mL
40 mM 0.0263 mL 0.1316 mL 0.2633 mL 0.6582 mL
50 mM 0.0211 mL 0.1053 mL 0.2106 mL 0.5266 mL
60 mM 0.0176 mL 0.0878 mL 0.1755 mL 0.4388 mL
80 mM 0.0132 mL 0.0658 mL 0.1316 mL 0.3291 mL
100 mM 0.0105 mL 0.0527 mL 0.1053 mL 0.2633 mL
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KB02-SLF Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

KB02-SLF2384184-40-9PROTACsFKBPFK506-binding proteinDegradermoleculargluecovalentlymodifyingDCAF16durabilityPROTAC-basedInhibitorinhibitorinhibit

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製品名:
KB02-SLF
製品番号:
HY-129610
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