2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. SIM1

SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.

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SIM1

SIM1 화학구조

CAS No. : 2719051-84-8

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg   견적 받기  
100 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of SIM1:

SIM1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SIM1

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity[1].

IC50 & Target

BRD2

1.1 nM (IC50)

BRD2

186 nM (Kd)

BRD3

 

BRD4

 

In Vitro

SIM1 (1 nM; 30 hours; MV4-11 cells) results in measurable cellular death after 6 hours[1].
SIM1 (1 μM; 4 hours; HEK293 cells) degrades BET proteins[1].
SIM1 induces conformational changes upon binding to the BET protein to simultaneously engage with high avidity both its bromodomains in a cis intramolecular fashion. SIM1 engages BD1 and BD2 intramolecularly and forms a 1:1:1 ternary complex with VHL and BRD4[1].

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

SIM1 Related Antibodies

Cell Viability Assay[1]

Cell Line: MV4-11 cells
Concentration: 1 nM
Incubation Time: 30 hours
Result: Resulted in measurable cellular death after 6 hours.

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 1 µM
Incubation Time: 4 hours
Result: Degraded BET proteins.
분자량

1618.81

화학식

C79H98Cl2N14O13S3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC1=C(C(C(C2=CC=C(C=C2)Cl)=N[C@@H](CC(NCCOCCOCCOCC(C)(COCCOCCOCCNC(C[C@@H]3N=C(C4=C(N5C3=NN=C5C)SC(C)=C4C)C6=CC=C(C=C6)Cl)=O)COCC(N[C@H](C(N7[C@@H](C[C@H](C7)O)C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)=O)C(C)(C)C)=O)=O)C%10=NN=C(C)N%11%10)=C%11S1)C
선적

Room temperature in continental US; may vary elsewhere.
보관

-20°C, protect from light, stored under nitrogen

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

용액&용해도
In Vitro: 

DMSO : 100 mg/mL (61.77 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 0.6177 mL 3.0887 mL 6.1774 mL
5 mM 0.1235 mL 0.6177 mL 1.2355 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 (protect from light, 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
순도&문서

Purity: 99.47%

SDS (252 KB)

COA (249 KB) HNMR (436 KB) LCMS (332 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 (protect from light, 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 0.6177 mL 3.0887 mL 6.1774 mL 15.4434 mL
5 mM 0.1235 mL 0.6177 mL 1.2355 mL 3.0887 mL
10 mM 0.0618 mL 0.3089 mL 0.6177 mL 1.5443 mL
15 mM 0.0412 mL 0.2059 mL 0.4118 mL 1.0296 mL
20 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
25 mM 0.0247 mL 0.1235 mL 0.2471 mL 0.6177 mL
30 mM 0.0206 mL 0.1030 mL 0.2059 mL 0.5148 mL
40 mM 0.0154 mL 0.0772 mL 0.1544 mL 0.3861 mL
50 mM 0.0124 mL 0.0618 mL 0.1235 mL 0.3089 mL
60 mM 0.0103 mL 0.0515 mL 0.1030 mL 0.2574 mL
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SIM1 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:

SIM12719051-84-8SIM 1SIM-1PROTACsEpigenetic Reader DomainpotentvonhippellindautrivalentPROTACpicomolaranti-cancerInhibitorinhibitorinhibit

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Inquiry Information

상품명:
SIM1
Cat. No.:
HY-141438
수량:
MCE Japan Authorized Agent:

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SAFETY DATA SHEET (SDS)

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